Lificiguat (YC-1)
中文名称：利非西呱
Lificiguat (YC-1)是一种不依赖于NO的soluble guanylyl cyclase(sGC)激活剂和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制剂。
Lificiguat (YC-1) Chemical Structure
CAS: 170632-47-0
产品质控
批次：
纯度：
99.94%
99.94
Lificiguat (YC-1)相关产品
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 |
|---|---|---|---|---|---|
| HT60 | Apoptosis assay | 26 uM | 48 hrs | Induction of apoptosis in HT60 cells at 26 uM after 48 hrs | 17189698 |
| HeLa | Function assay | 30 uM | 4 hrs | Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot | 19435661 |
| HCT116 | Function assay | 30 uM | 4 hrs | Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot | 19435661 |
| HCT116 | Function assay | 3 uM | Reduction of insulin-induced HIF-1 alpha expression in human HCT116 cells at 3 uM by western blot analysis | 27157007 | |
| HEK293 | Function assay | 16 hrs | Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay, IC50 = 9.21 μM. | 19435661 | |
| ACHN | Antitumor assay | 48 hrs | Antitumor activity against human ACHN cells after 48 hrs by MTT assay, IC50 = 0.3 μM. | 20097456 | |
| NCI-H226 | Antitumor assay | 48 hrs | Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay, IC50 = 1.9 μM. | 20097456 | |
| A498 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.37 μM. | 23831809 | |
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.27 μM. | 23831809 | |
| HeLa | Function assay | 12 hrs | Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay, IC50 = 1.5 μM. | 24900662 | |
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.2 μM. | 24900662 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.2 μM. | 24900662 | |
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50 = 29.3 μM. | 24900662 | |
| HT1080 | Proliferation assay | 72 hrs | Inhibition of cell proliferation of human HT1080 cells after 72 hrs by WST-8 dye based cell counting assay, IC50 = 30.9 μM. | 25773014 | |
| HT1080 | Function assay | 1 hr | Inhibition of HIF1 in human HT1080 cells transfected with 5xHRE/pGL3/VEGF/E1b reporter plasmid pre-incubated for 1 hr followed by incubation under hypoxia conditions for 24 hrs by HRE-driven luciferase reporter gene assay, IC50 = 48.4 μM. | 25773014 | |
| A498 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50 = 0.3 μM. | 26235951 | |
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells incubated for 48 hrs by MTT assay, IC50 = 25.27 μM. | 26235951 | |
| A498 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.3 μM. | 26820553 | |
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.3 μM. | 26820553 | |
| HeLa | Function assay | 12 hrs | Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay, IC50 = 1.2 μM. | 27847273 | |
| HeLa | Function assay | 12 hrs | Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay, IC50 = 2 μM. | ChEMBL | |
| U251HRE | Function assay | Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay, IC50 = 14.8 μM. | 18501601 | ||
| Hep3B | Function assay | Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay, IC50 = 13.8 μM. | 17884495 | ||
| AGS | Function assay | Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay, IC50 = 2 μM. | 17884495 | ||
| Hep3B | Function assay | Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay, IC50 = 13.8 μM. | 17328532 | ||
| AGS | Function assay | Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50 = 2 μM. | 17328532 | ||
| HL60 | Cytotoxicity assay | Cytotoxicity against HL60 cells by Propidium iodide exclusion assay, ED50 = 25.27 μM. | 17189698 | ||
| Sf21 | Function assay | Activation of sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO, EC50 = 4.11 μM. | 11141091 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by SRB assay, GI50 = 0.15849 μM. | ChEMBL | ||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by SRB assay, GI50 = 0.22387 μM. | ChEMBL | ||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by SRB assay, TGI = 0.52481 μM. | ChEMBL | ||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by SRB assay, TGI = 0.66069 μM. | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lificiguat (YC-1)是一种不依赖于NO的soluble guanylyl cyclase(sGC)激活剂和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制剂。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | YC-1是可溶性鸟苷酸环化酶（sGC）的变构激活剂。YC-1能增强该酶的催化速率，并使sGC对一氧化氮气体活化剂或一氧化碳敏感化。YC-1单独使用只能激活sGC10倍，但它能增强sGC依赖于CO和NO的激活效力，导致高度纯化的酶激活，其效力可达数百倍到数千倍[1]。在体外，YC-1能够抑制血小板聚集、血管收缩和HIF-1活性。YC-1可在转录后水平上完全抑制HIF-1α的表达，因此在低氧条件下抑制肝癌细胞中的HIF-1的转录因子活性，这说明YC-1的作用可能与氧传感通路相关，而不是sGC相关[2]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | Hep3B细胞 | ||
| 浓度 | 0.01-10 μM | |||
| 孵育时间 | 24 h | |||
| 方法 | 将Hep3B细胞以1 × 105细胞/孔的密度铺于6孔板中，加入含10%热灭活FBS的α-modified Eagle medium，培养过夜。然后用0.01-10 μM YC-1或DMSO处理细胞5分钟，然后置于常氧或低氧环境下24小时。测定VEGF水平。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | HO-1 / HO-2 HIF-1α p-ERK / p-p38 MAPK / p-JNK1 / p-AKT EZH2 / EZH1 / H3K27me3 / Histone H3 DNMT1 / DNMT3a / DNMT3b |
|
18923065 | |
| Growth inhibition assay | Cell proliferation Cell viability |
|
22507221 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 将YC-1作用于实验动物，导致富含血小板的血栓形成受到抑制、平均动脉血压降低(与cGMP水平上升相关)[1]。YC-1在负瘤小鼠中能有效地抑制肿瘤生长。YC-1处理过的小鼠肿瘤中HIF-1活性的抑制与血管生成、肿瘤生长受到抑制相关。而YC-1的抗血小板凝集效果并不影响肿瘤生长[2]。 | |
|---|---|---|
| 动物实验 | Animal Models | Male nude (BALB/cAnNCrj–nu/nu) mice |
| Dosages | 30 µg/g | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 304.34 | 分子式 | C19H16N2O2 |
| CAS号 | 170632-47-0 | SDF | Download Lificiguat (YC-1) SDF |
| Smiles | C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 61 mg/mL ( (200.43 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 31 mg/mL (101.85 mM) Water : Insoluble |
摩尔浓度计算器 |
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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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