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R 268712

Catalog #: 5288 1 Review Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5288/50
5288/10
R 268712 | CAS No. 879487-87-3 | TGF-beta Receptor Inhibitors
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Description: Potent and selective inhibitor of TGF-βRI

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

Purity: ≥98%

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Biological Activity

R 268712 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Inhibition of pSmad 2/3 in a human epithelial cell line
By Anonymous on 10/26/2020
Species: Human

Tested a human lung epithelial cell line pretreated with R268712 at either 10, 1 or 0.1uM for 30 min and then added TGFb1 at 5ng/ml in two different matrices. Incubated 24hr and then lysed cells to look at pSmad 2/3 levels by immunoassay

Inhibition of pSmad 2/3 in a human epithelial cell line 5288
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