Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
G649634-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $50.90 | |
G649634-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $105.90 | |
G649634-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $178.90 | |
G649634-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $255.90 | |
G649634-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $390.90 |
Specifications & Purity | 99% |
---|---|
Storage Temp | Store at -20°C |
Shipped In | Dry ice |
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. Form:Solid 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) |
---|
IUPAC Name | 4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide |
---|---|
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) |
InChi Key | KZYAHEIPPAPADQ-UHFFFAOYSA-N |
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 |
Isomeric 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 |
PubChem CID | 11548023 |
Molecular Weight | 513.33 |
Enter Lot Number to search for COA:
Solubility | DMSO : 50 mg/mL (97.40 mM; Need ultrasonic) |
---|