An inhibitor of ALK5
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R-268712

Item No. 36810

Technical Information
Formal Name
4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
CAS Number
879487-87-3
Molecular Formula
C20H18FN5O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 10 mg/mlEthanol: 20 mg/ml
λmax
230, 252, 290 nm
SMILES
FC(C=C1)=C(C2=CN(CCO)N=C2)C=C1C3=CNN=C3C4=NC(C)=CC=C4
InChi Code
InChI=1S/C20H18FN5O/c1-13-3-2-4-19(24-13)20-17(11-22-25-20)14-5-6-18(21)16(9-14)15-10-23-26(12-15)7-8-27/h2-6,9-12,27H,7-8H2,1H3,(H,22,25)
InChi Key
JQGOCCALXFSRHZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    R-268712 is an inhibitor of activin receptor-like kinase (ALK5; IC50 = 2.5 nM).1 It is selective for ALK5 over p38 MAPK (IC50 = 12 µM). R-268712 (1, 3, and 10 mg/kg) reduces renal fibrosis in a model of unilateral ureteral obstruction using transgenic Col1a1-Luc Tg rats, a reporter model for collagen I expression. It also reduces proteinuria and glomerulosclerosis and improves renal function in heminephrectomized rats in a model of glomerulonephritis using antibodies against Thy-1 membrane glycoprotein when administered at doses of 0.3 and 1 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. H., T., M., K., M., E., et alR-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur. J. Pharmacol. 734, 60-66 (2014).