GSK269962A HCl

别名: GSK269962B, GSK269962

GSK269962A HCl是选择性的ROCK(Rho-associated protein kinase)抑制剂,对ROCK1和ROCK2的IC50分别为1.6 nM和4 nM。

GSK269962A HCl Chemical Structure

GSK269962A HCl Chemical Structure

CAS: 2095432-71-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 958.23 现货
5mg 794.65 现货
25mg 3252.41 现货
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GSK269962A HCl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(PMID)
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=18.8477 μM
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=24.8749 μM
NCI-H1963 Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=1.27839 μM
NCI-H2081 Growth inhibition assay Inhibition of human NCI-H2081 cell growth in a cell viability assay, IC50=34.6044 μM
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=22.6272 μM
NCI-H2107 Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=25.6561 μM
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=6.50426 μM
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=0.95937 μM
NCI-H2227 Growth inhibition assay Inhibition of human NCI-H2227 cell growth in a cell viability assay, IC50=7.88616 μM
NCI-H524 Growth inhibition assay Inhibition of human NCI-H524 cell growth in a cell viability assay, IC50=22.8763 μM
NCI-H526 Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=18.5431 μM
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=2.45161 μM
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=15.0578 μM
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.82294 μM
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=10.9496 μM
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=17.201 μM
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.9191 μM
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=46.195 μM
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=8.71808 μM
P30-OHK cell Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=7.62877 μM
P30-OHK cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=7.04954 μM
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.22126 μM
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=0.49004 μM
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=18.9036 μM
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=10.5662 μM
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=10.67 μM
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=18.5236 μM
RPMI-8402 cell Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=4.5856 μM
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.393 μM
Ramos-2G6-4C10 cell Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.357 μM
SCLC-21H cell Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=7.61149 μM
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=11.8321μM
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=6.23183 μM
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=1.28661 μM
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=5.75508 μM
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=11.7259 μM
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.04526 μM
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=32.5965 μM
SK-MM-2 cell Growth inhibition assay Inhibition of human SK-MM-2 cell growth in a cell viability assay, IC50=42.3405 μM
SK-N-DZ cell Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.48314 μM
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=17.5456 μM
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=24.9736 μM
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=8.07737 μM
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=0.000137 μM
SU-DHL-1 cell Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=12.7336 μM
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=39.011 μM
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.88656 μM
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50=12.7521 μM
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM
AM-38 cell Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=7.26327 μM
ATN-1 cell Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=24.7555 μM
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=22.2532 μM
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.00789 μM
human BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=3.97107 μM
BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.14081μM
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=3.40703 μM
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=18.8859 μM
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=13.9545 μM
CAL-148 cell Growth inhibition assay Inhibition of human CAL-148 cell growth in a cell viability assay, IC50=35.6557 μM
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=22.8423 μM
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=32.4114 μM
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=11.6089 μM
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=36.6381 μM
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50=23.3577 μM
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=8.70625 μM
WSU-NHL cell Growth inhibition assay Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=27.1907 μM
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=0.66846 μM
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50=47.0263 μM
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=0.847 μM
CCRF-CEM cell Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=8.65392 μM
CMK cell Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50=1.01323 μM
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=3.24226 μM
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=2.0738 μM
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=36.5497 μM
CRO-AP2 cell Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=2.36088 μM
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=23.9145 μM
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=47.586 μM
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=0.62814 μM
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=0.08509 μM
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.62854 μM
D-392MG cell Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=1.43039 μM
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=8.53492 μM
D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=12.3152 μM
DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=47.1417 μM
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=7.01898 μM
DMS-114 cell Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=49.8468 μM
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=42.9923 μM
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=4.22764 μM
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=8.43623 μM
Daudi cell Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=2.09802 μM
EC-GI-10 cell Growth inhibition assay Inhibition of human EC-GI-10 cell growth in a cell viability assay, IC50=44.2589 μM
ECC4 cell Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=32.1896 μM
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=2.45594 μM
ES1 cell Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=5.54087 μM
ES3 cell Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=42.4729 μM
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50=35.195 μM
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=0.24733 μM
ES7 cell Growth inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50=5.23124 μM
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.81924 μM
EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=13.6759 μM
EW-22 cell Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=47.7947 μM
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50=9.80389 μM
GDM-1 cell Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=8.39196 μM
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=0.00523 μM
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=0.04951 μM
GR-ST cell Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50=13.7902 μM
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50=1.60389 μM
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=6.69712 μM
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=37.6011 μM
HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=13.3834 μM
HD-MY-Z cell Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=25.2146 μM
HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=12.2114 μM
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=23.9527 μM
HT cell Growth inhibition assay Inhibition of human HT cell growth in a cell viability assay, IC50=4.44321 μM
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=4.90686 μM
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=3.78986 μM
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=32.9086 μM
IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=2.17079 μM
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=3.26608 μM
K052 cell Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50=0.75301 μM
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=33.5915 μM
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=29.3969 μM
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=42.9142 μM
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=4.11247 μM
KE-37 cell Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.835 μM
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=23.9757 μM
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=0.56742 μM
KM12 cell Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=3.52964 μM
KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=30.4549 μM
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay, IC50=8.81915 μM
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=37.426 μM
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.0046 μM
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=23.484 μM
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=20.7445 μM
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=13.6742 μM
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=28.3883 μM
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=10.5536 μM
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=1.71496μM
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=11.1726 μM
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=12.7431 μM
LC4-1 cell Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=32.8341 μM
LOUCY cell Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50=1.15276 μM
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.2122 μM
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=39.2258 μM
LU-134-A cell Growth inhibition assay Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=7.14068 μM
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=22.218 μM
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=17.4351μM
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=45.0841 μM
MDA-MB-134-VI cell Growth inhibition assay Inhibition of human MDA-MB-134-VI cell growth in a cell viability assay, IC50=39.2486 μM
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.64383 μM
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=0.0669 μM
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=3.40304 μM
MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=4.43653 μM
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=4.11163 μM
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=14.4124 μM
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=1.25922 μM
MRK-nu-1 cell Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=0.57572 μM
MSTO-211H cell Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=12.869 μM
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.13915 μM
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=1.56109 μM
NB1 cell Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=3.84369 μM
NB10 cell Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50=0.13915 μM
NB12 cell Growth inhibition assay Inhibition of human NB12 cell growth in a cell viability assay, IC50=16.5656 μM
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=2.31278 μM
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=3.58051 μM
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=0.59114 μM
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50=41.8453 μM
NCI-H1155 cell Growth inhibition assay Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50=14.3408 μM
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay, IC50=11.8982 μM
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.9411 μM
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=22.8795 μM
NCI-H1417 cell Growth inhibition assay Inhibition of human NCI-H1417 cell growth in a cell viability assay, IC50=5.67522 μM
NCI-H1436 cell Growth inhibition assay Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50=3.84101 μM
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=12.8935 μM
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=36.6284 μM
点击查看更多细胞系数据

生物活性

产品描述 GSK269962A HCl是选择性的ROCK(Rho-associated protein kinase)抑制剂,对ROCK1和ROCK2的IC50分别为1.6 nM和4 nM。
靶点
ROCK1 [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
MSK1 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
1.6 nM 4 nM 49 nM 132 nM
体外研究(In Vitro)
体外研究活性 GSK269962A在人类平滑肌中,完全阻断血管紧张肽Ⅱ诱导的肌动蛋白张力丝的形成。这一抑制现象始于约1 μM GSK269962A。GSK269962A在预束紧的大鼠动脉(组织浴/组织培养)中诱导血管舒张,IC50为35 nM。GSK269962A所诱导的舒张是可逆的。GSK269962A在巨噬细胞中抑制IL-6 mRNA的转录、减少LPS诱导的IL-6和TNF-α蛋白的产生[1]
细胞实验 细胞系 平滑肌细胞
浓度 3 μM
孵育时间 150 min
方法 对人类平滑肌细胞进行血清饥饿处理(细胞于盖玻片上生长,达到50%融合时,血清饥饿处理过夜),用AngⅡ(100 nM)对其进行刺激2小时。在刺激前30分钟,加入ROCK抑制剂(3 μM SB-772077-B或GSK269962A),刺激后将细胞进行固定,用鬼笔环肽对肌动蛋白进行染色。
体内研究(In Vivo)
体内研究活性 自发性高血压大鼠口服GSK269962A将降低体循环血压,血压的减少非常迅速并显著。在口服给药后约2小时,其降血压作用达到峰值。血压的减少伴随着急性、剂量依赖性的心率增加,这可能是压力反射机制的激活[1]。用10 mg/kg的GSK 269962抑制ROCK在大鼠内能依次地引起排尿量、排尿后残余尿、容量阈值、泌尿效率、ICI(intercontraction interval)、膀胱顺应性、VTNVC的升高,而对心率、收缩压、平均血压、舒张压没有影响[2]
动物实验 Animal Models Wistar雌性大鼠
Dosages 5 或 10 mg/kg
Administration 动脉注射
  • https://pubmed.ncbi.nlm.nih.gov/17018693/
  • http://onlinelibrary.wiley.com/doi/10.1002/nau.22978/abstract

化学信息&溶解度

分子量 607.06 分子式

C29H30N8O5.HCl

CAS号 2095432-71-4 SDF Download GSK269962A HCl SDF
Smiles CCN1C2=CC(=NC=C2N=C1C3=NON=C3N)OC4=CC=CC(=C4)NC(=O)C5=CC=C(C=C5)OCCN6CCOCC6.Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (164.72 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 28 mg/mL (46.12 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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