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Product Name:GSK269962A hydrochloride
CAS:2095432-71-4
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| | GSK269962 Hydrochloride Basic information |
| Product Name: | GSK269962 Hydrochloride | | Synonyms: | GSK269962 Hydrochloride;GSK269962 HCl;GSK269962A hydrochloride;N-(3-((2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl)oxy)phenyl)-4-(2-morpholinoethoxy)benzamide hydrochloride;GSK269962A HCl ，S7687 | | CAS: | 2095432-71-4 | | MF: | C29H31ClN8O5 | | MW: | 607.07 | | EINECS: | | | Product Categories: | | | Mol File: | 2095432-71-4.mol |  |
| | GSK269962 Hydrochloride Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 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 |
| | GSK269962 Hydrochloride Usage And Synthesis |
| 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 |
| | GSK269962 Hydrochloride Preparation Products And Raw materials |
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