R 268712
Chemical Name: 4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
Purity: ≥98%
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
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.
Background References
-
R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model.
Terashima et al.
Eur.J.Pharmacol., 2014;734:60
Product Datasheets
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for R 268712
Average Rating: 5 (Based on 1 Review)
Have you used R 268712?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Filter by:
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
