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R-268712
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Purity:99.77%
R-268712
Catalog No. T16708Cas No. 879487-87-3
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | 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 |
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CitedProduct Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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Keywords
renal fibrosisThy1 nephritisTransforming growth factor beta receptorsglomerulonephritisTransforming growth factor betaALK tyrosine kinase receptorHFL-1glomerulosclerosisCD246InhibitorCluster of differentiation 246R 268712UUOAnaplastic lymphoma kinase (ALK)R-268712inhibitTGF-βR268712TGF-beta/SmadCKDTGF-β ReceptorAnaplastic lymphoma kinase
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