R 268712

Modify Date: 2024-02-01 18:52:27

R 268712 Structure
R 268712 structure
Common Name R 268712
CAS Number 879487-87-3 Molecular Weight 363.388
Density 1.3±0.1 g/cm3 Boiling Point 576.8±50.0 °C at 760 mmHg
Molecular Formula C20H18FN5O Melting Point N/A
MSDS N/A Flash Point 302.7±30.1 °C

 Use of R 268712


R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: ALK5in 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. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]

 Names

Name R-268712
Synonym More Synonyms

 R 268712 Biological Activity

Description R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: ALK5in 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. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]
Related Catalog
References

[1]. Terashima H, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 576.8±50.0 °C at 760 mmHg
Molecular Formula C20H18FN5O
Molecular Weight 363.388
Flash Point 302.7±30.1 °C
Exact Mass 363.149536
LogP 2.79
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.675
Storage condition 2-8℃

 Synonyms

1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[5-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-
2-(4-{2-Fluoro-5-[5-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl}-1H-pyrazol-1-yl)ethanol