GSK-25

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).

Product information

CAS Number: 874119-56-9

Molecular Weight: 513.33

Formula: C24H16Cl2F2N6O

Chemical Name: GSK-25

Smiles: CC1NC(=NC(C=1C(=O)NC1C=C2C=NNC2=CC=1F)C1=CC=C(Cl)C=C1F)C1=CC(Cl)=NC=C1

InChiKey: KZYAHEIPPAPADQ-UHFFFAOYSA-N

InChi: InChI=1S/C24H16Cl2F2N6O/c1-11-21(24(35)32-19-6-13-10-30-34-18(13)9-17(19)28)22(15-3-2-14(25)8-16(15)27)33-23(31-11)12-4-5-29-20(26)7-12/h2-10,22H,1H3,(H,30,34)(H,31,33)(H,32,35)

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO: 100 mg/mL (194.81 mM)

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: ≥360 days 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:

GSK-25 (Rat aorta IC50=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure. GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey).

References:

1. Sehon CA, et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4.

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