GSK-25


Catalog No. size PriceQuantity
M6874-2 2mg solid $104
M6874-10 10mg solid $401

Description

Cas:874119-56-9

Product Information

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).

 

IC50 & Target:

ROCK1   7 nM (IC50)

RSK1     398 nM (IC50)

p70S6K   1000 nM (IC50)

 

Molecular Weight:513.33

 

Chemical Formula: C₂₄H₁₆Cl₂F₂N₆O

Smiles Code:

 

ClC1=CC(C2=NC(C3=C(F)C=C(Cl)C=C3)C(C(NC4=C(F)C=C(NN=C5)C5=C4)=O)=C(C)N2)=CC=N1

 

Shipping:

Room temperature in continental US; may vary elsewhere.

 

Storage Condition:

 

Powder     -20°C  3 years

4°C  2 years

In solvent -80°C  6 months

-20°C  1 month

 

 

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.

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