| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: 100 mg/mL (164.73 mM);Ethanol: 28 mg/mL (46.12 mM) | [form ]
Solid | [color ]
Off-white to light yellow | [Water Solubility ]
Water: Insoluble |
| Hazard Information | Back Directory | [Uses]
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities[1]. | [Biological Activity]
GSK269962A HCl is a selective ROCK (Rho-associated protein kinase) inhibitor with IC50 of 1.6 nM and 4 nM for ROCK1 and ROCK2, respectively. | [in vivo]
GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial[1]. | Animal Model: | Male Sprague-Dawley rats (350-400g)[1] | | Dosage: | 0.3, 1, and 3 mg/kg | | Administration: | Oral gavage; 12 hours | | Result: | Induced a dose-dependent reduction in blood pressure. |
| [target]
| Target | Value | ROCK1
(Cell-free assay) | 1.6 nM | ROCK2
(Cell-free assay) | 4 nM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> MSK1
(Cell-free assay) 49 nM | RSK1
(Cell-free assay) | 132 nM |
| [IC 50]
ROCK1: 1.6 nM (IC50); ROCK2: 4 nM (IC50); RSK1: 132 nM (IC50); MSK1: 49 nM (IC50); AKT1: 955 nM (IC50); AKT2: 1350 nM (IC50); AKT3: 1510 nM (IC50); CDK2: 3500 nM (IC50); GSK3α: 1260 nM (IC50) | [References]
[1] Doe C, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. DOI:10.1124/jpet.106.110635 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|