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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G655933-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $119.90 |
Specifications & Purity | 10mM in DMSO |
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Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product Description | GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor ( IC 50 =7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC 50 =398 nM, p70S6K: IC 50 =1 μM). GSK-25 inhibits P450 profile (IC 50 s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) In Vivo GSK-25 (Rat aorta IC 50 =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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:ROCK1 7 nM (IC 50 ) RSK1 398 nM (IC 50 ) p70S6K 1000 nM (IC 50 ) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | CC1=C(C(N=C(N1)C2=CC(=NC=C2)Cl)C3=C(C=C(C=C3)Cl)F)C(=O)NC4=C(C=C5C(=C4)C=NN5)F |
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Molecular Weight | 513.33 |
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