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R-268712

Chemical Structure : R-268712

CAS No.: 879487-87-3

R-268712 (R268712;R 268712)

Catalog No.: PC-43290Not For Human Use, Lab Use Only.

R-268712 is a potent, selective, orally active inhibitor of TGF-β type I receptor ALK5 with IC50 of 2.5 nM, >5,000-fold more selectivity than p38 MAPK.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

R-268712 is a potent, selective, orally active inhibitor of TGF-β type I receptor ALK5 with IC50 of 2.5 nM, >5,000-fold more selectivity than p38 MAPK; inhibits the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model at doses of 1, 3 and 10mg/kg, also reduces proteinuria and glomerulosclerosis significantly with improvement of renal function in glomerulonephritis models.

Physicochemical Properties

M.Wt 363.3882
Formula C20H18FN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-

References

1. Terashima H, et al. Eur J Pharmacol. 2014 Jul 5;734:60-6.

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