GSK269962

GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively. GSK269962 can become an alternative worth considering in OAB treatment.

Product information

CAS Number: 850664-21-0

Molecular Weight: 570.60

Formula: C29H30N8O5

Synonym:

GSK269962A

GSK269962B

Related CAS Number:

925213-80-5 (3HCl)

2095432-71-4 (HCl)

Chemical Name: 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-(4-morpholinyl)ethoxy]-benzamide

Smiles: CCN1C(=NC2=CN=C(C=C12)OC1=CC(=CC=C1)NC(=O)C1C=CC(=CC=1)OCCN1CCOCC1)C1=NON=C1N

InChiKey: YOVNFNXUCOWYSG-UHFFFAOYSA-N

InChi: InChI=1S/C29H30N8O5/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM.

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.

References:

1. Hutchinson JL, Rajagopal SP, Yuan M, Norman JE. Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways. FASEB J. 2014 Jan;28(1):94-105. doi: 10.1096/fj.13-237040. Epub 2013 Sep 27. PubMed PMID: 24076962.
2. Doe C, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.

Products are for research use only. Not for human use.