Melatonin
别名: NSC 56423, N-Acetyl-5-methoxytryptamine,NSC 113928,MT 中文名称：褪黑素
Melatonin是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。
Melatonin Chemical Structure
CAS: 73-31-4
产品质控
批次：
纯度：
99.95%
99.95
Melatonin相关产品
| 相关靶点 | MT1 receptor MT2 receptor | 点击展开 |
|---|---|---|
| 相关产品 | Luzindole | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I GPCR小分子化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| PC12 | Neuroprotective assay | 25 uM | 2 hrs | Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 28800459 |
| PC12 | Neuroprotective assay | 20 uM | 24 hrs | Neuroprotective activity against amyloid beta (1 to 42 residues) induced cell death in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 24 hrs followed by amyloid beta (1 to 42 residues) addition measured after 24 hrs by MTT | 27484514 |
| PC12 | Neuroprotective assay | 10 uM | 2 hrs | Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay | 27460699 |
| SH-SY5Y | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against H2O2-induced oxidative stress-associated death in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 24 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay | 26363866 |
| Primary neural stem cells | Neurogenic assay | 10 uM | 48 hrs | Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring MAP-2 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry | 24738476 |
| Primary neural stem cells | Neurogenic assay | 10 uM | 48 hrs | Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring TuJ1 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry | 24738476 |
| NIH3T3 | Function assay | 1 nM | Activity at MT1 receptor expressed in NIH3T3 cells assessed as inhibition of forskolin-stimulated cAMP synthesis at 1 nM | 16759094 | |
| CHO | Function assay | 1 hr | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00095μM | 31727472 | |
| COS7 | Function assay | 1.5 hrs | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00088μM | 31727472 | |
| CHO | Function assay | 1 hr | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00046μM | 31727472 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.0002042μM | 31727472 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.000302μM | 31727472 | |
| COS7 | Function assay | 1.5 hrs | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00018μM | 31727472 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.9μM | 29144746 | |
| CHO | Function assay | 60 mins | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method, IC50=0.00011μM | 27876250 | |
| HEK293 | Function assay | 120 mins | Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00034μM | 26785296 | |
| HEK293 | Function assay | 120 mins | Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00025μM | 26785296 | |
| HEK293 | Function assay | 120 mins | Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00041μM | 25232966 | |
| HEK293 | Function assay | 120 mins | Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00014μM | 25232966 | |
| CHO | Function assay | 1 hr | Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0017μM | 24417958 | |
| CHO | Function assay | 1 hr | Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0004μM | 24417958 | |
| CHOK1 | Function assay | 3 hrs | Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.00021μM | 23403082 | |
| CHOK1 | Function assay | 3 hrs | Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, Ki=0.00011μM | 23403082 | |
| HEK293 | Function assay | 2 hrs | Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0005μM | 23265885 | |
| HEK293 | Function assay | 2 hrs | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0002μM | 23265885 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000429μM | 23228808 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000296μM | 23228808 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003388μM | 22047556 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.000263μM | 22047556 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.00082μM | 21568291 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.000026μM | 21568291 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0008511μM | 21473625 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0000257μM | 21473625 | |
| CHO-Galpha16 | Function assay | 20 mins | Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.0011μM | 21237644 | |
| CHO-Galpha16 | Function assay | 20 mins | Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.00056μM | 21237644 | |
| NIH3T3 | Function assay | 90 mins | Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0006166μM | 20674373 | |
| NIH3T3 | Function assay | 90 mins | Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003311μM | 20674373 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000429μM | 20227878 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000296μM | 20227878 | |
| CHO | Function assay | 1 hr | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.0004571μM | ChEMBL | |
| CHO | Function assay | 1 hr | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.000955μM | ChEMBL | |
| NIH3T3 | Function assay | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00066μM | 31727472 | ||
| NIH3T3 | Function assay | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00033μM | 31727472 | ||
| HEK293 | Function assay | Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.025μM | 31204226 | ||
| HEK293 | Function assay | Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.001μM | 31204226 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| CHO | Function assay | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells, IC50=0.00011μM | 26988801 | ||
| HEK293 | Function assay | Displacement of [125L]iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00041μM | 24930835 | ||
| HEK293 | Function assay | Displacement of [125L]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM | 24930835 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00034μM | 21764185 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00025μM | 21764185 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00024μM | 21568291 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00021μM | 21568291 | ||
| CHO | Function assay | Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting, Ki=0.00024μM | 21473625 | ||
| CHO | Function assay | Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting, Ki=0.00021μM | 21473625 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0015μM | 21420861 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00042μM | 21420861 | ||
| HEK293 | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00034μM | 21420861 | ||
| HEK293 | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00025μM | 21420861 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00035μM | 21392858 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00022μM | 21392858 | ||
| CHO-Galpha16 | Function assay | Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells, Ki=0.00099μM | 21237644 | ||
| CHO-Galpha16 | Function assay | Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells, Ki=0.00058μM | 21237644 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0022μM | 20444610 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00049μM | 20444610 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting, Ki=0.0004571μM | 19473848 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting, Ki=0.000955μM | 19473848 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00224μM | 19329323 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00049μM | 19329323 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM | 19193160 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM | 19193160 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay, EC50=0.00049μM | 18778943 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00041μM | 18778943 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM | 18778943 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells, Ki=0.000741μM | 18657980 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells, Ki=0.000525μM | 18657980 | ||
| CHO | Function assay | Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells, IC50=0.06457μM | 18400335 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells, IC50=0.00053μM | 18372181 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, IC50=0.0002μM | 18372181 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0002399μM | 18052314 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0001413μM | 18052314 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0003μM | 17481904 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0002μM | 17481904 | ||
| NIH3T3 | Function assay | Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.0003388μM | 17459711 | ||
| NIH3T3 | Function assay | Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.000263μM | 17459711 | ||
| NIH 3T3 | Function assay | Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells, Ki=0.000389μM | 17346859 | ||
| NIH 3T3 | Function assay | Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells, Ki=0.0003548μM | 17346859 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells, Ki=0.000257μM | 17149869 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells, Ki=0.0003236μM | 17149869 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.00039μM | 16759094 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.00035μM | 16759094 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells , Ki=0.0002818μM | 15943478 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells, Ki=0.0002884μM | 15943478 | ||
| NIH3T3 | Function assay | Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0007μM | 15713384 | ||
| NIH3T3 | Function assay | Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0003μM | 15713384 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0007μM | 15380218 | ||
| NIH3T3 | Function assay | Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells, Ki=0.0002884μM | 15293992 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0003μM | 15380218 | ||
| NIH3T3 | Function assay | Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells, Ki=0.0002818μM | 15293992 | ||
| NIH3T3 | Function assay | Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0004μM | 14980664 | ||
| NIH3T3 | Function assay | Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0003μM | 14980664 | ||
| NIH3T3 | Function assay | Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells., Ki=0.0004μM | 14643330 | ||
| NIH3T3 | Function assay | Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells, Ki=0.0003μM | 14643330 | ||
| HEK293 | Function assay | Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00041μM | 12646022 | ||
| HEK293 | Function assay | Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00014μM | 12646022 | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells, Ki=0.0000823μM | 12213063 | ||
| CHO | Function assay | Ability to inhibit 2-[125I]iodomelatonin specific binding to human melatonin receptor type 1A (MT1) expressed in CHO cells., Ki=0.0000823μM | 12213062 | ||
| CHO | Function assay | Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A, EC50=0.00192μM | 12061881 | ||
| CHO | Function assay | Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells, EC50=0.00047μM | 12061881 | ||
| HEK293 | Function assay | Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand., Ki=0.00031μM | 12061881 | ||
| HEK293 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells, Ki=0.00031μM | 11960497 | ||
| HEK293 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells, Ki=0.00012μM | 11960497 | ||
| NIH 3T3 | Function assay | Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand, Ki=0.0002884μM | 11520198 | ||
| NIH 3T3 | Function assay | Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin, Ki=0.0002818μM | 11520198 | ||
| HEK293 | Function assay | Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.00053μM | 11063602 | ||
| HEK293 | Function assay | Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.0002μM | 11063602 | ||
| NIH 3T3 | Function assay | Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00066μM | 10737738 | ||
| NIH 3T3 | Function assay | Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00033μM | 10737738 | ||
| NIH3T3 | Function assay | Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells, Ki=0.0002951μM | 9733487 | ||
| CHO | Function assay | Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=0.00008μM | 9435890 | ||
| CHO | Function assay | Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1B expressed in CHO cells, Ki=0.00012μM | 9435890 | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00013μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells, Ki=0.0002μM | ChEMBL | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00023μM | ChEMBL | ||
| CHO | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells, Ki=0.00029μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells by Gamma counting, Ki=0.0004571μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells by Gamma counting, Ki=0.000955μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Melatonin是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Melatonin与高毒性羟基自由基相互作用，数率常数等于其他高效羟基自由基清除剂。Melatonin被报到能够中和过氧化氢，单线态氧，过氧亚硝基阴离子，一氧化氮和次氯酸。[1] Melatonin被认为能够清除高毒性羟基自由基，过氧亚硝酸盐阴离子，可能也作用于氢过氧自由基。据报道，Melatonin清除超氧阴离子自由基，并且能够淬灭单线态氧。Melatonin刺激超氧化物歧化酶的mRNA水平，并活化谷胱甘肽过氧化物酶，谷胱甘肽还原酶和葡萄糖-6-磷酸脱氢酶(都为抗氧化酶)，从而增加其抗氧化能力。[2] 在体外，Melatonin在无细胞体系中被证实能够直接清除H2O2，单线态氧(1O2)和一氧化氮(NO*)，几乎或完全没有清除超氧阴离子自由基(O2*-)的能力。Melatonin也能够直接作用于过氧亚硝基阴离子(ONOO-)和/或过氧亚硝酸(ONOOH)，或该分子的活化形式，ONOOH*，使它们失去毒性。Melatonin作为一种直接自由基清除剂，具有清除活性氧和活性氮自由基毒性的能力。[3] Melatonin抑制大部分检测细胞中的cAMP积累，但至今为止，对其它信使吲哚基的作用仅在一种类型的细胞或组织中经常观察到。Melatonin也能够调节转录因子，即cAMP响应元件结合蛋白的磷酸化和c-Fos的表达。[4] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | MT1 / MT2 / p-CREB / CREB / BDNF p-Raf / p-ERK / p-p90RSK / PKAα / p-AKT / p-JNK / p-CaMKII |
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29570621 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04521972 | Not yet recruiting | Pregnancy Related|Labor; Poor|Uterine Contractions Weak |
Michigan State University|McLaren Health Care |
October 1 2024 | Not Applicable |
| NCT06390267 | Not yet recruiting | Acute Stress Reaction|Cognitive Performance |
Spark Biomedical Inc.|Battelle Memorial Institute |
August 2024 | Not Applicable |
| NCT06343805 | Not yet recruiting | Primary Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|PMF|PPV-MF|PET-MF |
Ajax Therapeutics Inc. |
July 15 2024 | Phase 1 |
化学信息&溶解度
| 分子量 | 232.28 | 分子式 | C13H16N2O2 |
| CAS号 | 73-31-4 | SDF | Download Melatonin SDF |
| Smiles | CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 47 mg/mL ( (202.34 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 47 mg/mL (202.34 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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