R 268712

Cat. No. 5288

R 268712 C20H18FN5O [879487-87-3]

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Chemical Name: 4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol

Biological Activity

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, glomerulosclerosis and improves renal function in an anti-Thy1 glomerulonephritis model. Orally bioavailable.

Technical Data

M.Wt:
363.39
Formula:
C20H18FN5O
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
879487-87-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Terashima et al (2014) R-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. PMID: 24726873.

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Keywords: R 268712, supplier, R268712, potent, selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1, ALK5, ALK, receptors, activin, receptor-like, Kinases, transforming, growth, factor, β, kidney, Tocris Bioscience, TGF-β Receptor Inhibitor products

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