GSK269962


Catalog No. size PriceQuantity
M6850-2 2mg solid $81
M6850-10 10mg solid $324

Description

Cas:850664-21-0

Product Information

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.

 

Chemical Formula: C29H30N8O5

 

Exact Mass: 570.2339

 

Molecular Weight: 570.61

 

Elemental Analysis: C, 61.04; H, 5.30; N, 19.64; O, 14.02

 

Related CAS #: 

925213-80-5 (3HCl)   

850664-21-0 (free base)   2

095432-71-4 (HCl)    

 

Synonym:

 

GSK269962A

GSK269962B

 

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

 

InChi Key:

YOVNFNXUCOWYSG-UHFFFAOYSA-N

 

InChi Code: 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)

 

Smiles Code:

O=C(NC1=CC=CC(OC2=CC3=C(N=C(C4=NON=C4N)N3CC)C=N2)=C1)C5=CC=C(OCCN6CCOCC6)C=C5

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  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.

 

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

 

 

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