GSK269962 HCl

Modify Date: 2024-01-22 20:45:53

GSK269962 HCl Structure
GSK269962 HCl structure
Common Name GSK269962 HCl
CAS Number 2095432-71-4 Molecular Weight 607.06
Density N/A Boiling Point N/A
Molecular Formula C29H31ClN8O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK269962 HCl


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].

 Names

Name GSK269962A hydrochloride

 GSK269962 HCl Biological Activity

Description 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].
Related Catalog
Target

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)

In Vitro GSK269962A has an IC50 of 1.6 nM toward recombinant human ROCK1. GSK269962A exhibits more than 30-fold selectivity against a panel of serine/threonine kinases[1]. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM[1].
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.
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.

 Chemical & Physical Properties

Molecular Formula C29H31ClN8O5
Molecular Weight 607.06