R-268712
Cat. No.: DC8022
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Chemical Structure
879487-87-3
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Field of application
Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler
| Cas No.: |
879487-87-3 |
| Chemical Name: |
4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol |
| Synonyms: |
R 268712,R268712 |
| SMILES: |
FC1C=CC(C2C(C3N=C(C)C=CC=3)=NNC=2)=CC=1C1C=NN(CCO)C=1 |
| Formula: |
C20H18FN5O |
| M.Wt: |
363.39 |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. |
| In Vivo: |
Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1] |
| In Vitro: |
R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1] |
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