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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $44 | In Stock | |
2 mg | $64 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $168 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $588 | In Stock | |
100 mg | $838 | In Stock | |
1 mL x 10 mM (in DMSO) | $116 | In Stock |
Description | R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor. |
In vitro | R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor.?Evaluation of in vitro inhibition indicated that R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). |
In vivo | Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model.?Additionally, the efficacy of R-268712 in a heminephrectomized anti-Thy1 glomerulonephritis model at doses of 0.3 and 1mg/kg.?R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function. |
Molecular Weight | 363.39 |
Formula | C20H18FN5O |
Cas No. | 879487-87-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 110 mg/mL (302.7 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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