GSK-25
GSK-25 Basic information
- Product Name:
- GSK-25
- Synonyms:
-
- 4-(4-Chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide
- GSK-25
- 5-PyriMidinecarboxaMide, 4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-Methyl-
- 4-(4-Chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4
- GSK25;GSK 25
- 4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide
- Rho-associated kinase,ROK,ROCK,Rho-associated protein kinase,S6K,bioavailable,Ribosomal S6 Kinase (RSK),Rho-kinase,Inhibitor,p70S6K,selective,pressure,P450,inhibit,GSK-25,GSK 25,blood,orally
- 4-(4-Chloro-2-fluorophenyl)-2-(2-chloro-4-pyridyl)-N-(6-fluoro-5-indazolyl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide
- CAS:
- 874119-56-9
- MF:
- C24H16Cl2F2N6O
- MW:
- 513.33
- Mol File:
- 874119-56-9.mol
GSK-25 Chemical Properties
- Boiling point:
- 751.7±60.0 °C(Predicted)
- Density
- 1.57±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 100 mg/mL (194.81 mM)
- form
- Solid
- pka
- 11.61±0.40(Predicted)
- color
- Light yellow to yellow
GSK-25 Usage And Synthesis
Uses
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)[1].
in vivo
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[1].
?
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)[1].
IC 50
ROCK1: 7 nM (IC50); RSK1: 398 nM (IC50); p70S6K: 1000 nM (IC50)
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. DOI:10.1021/jm8005096
GSK-25Supplier
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