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R-268712

Catalog No. T16708 CAS 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.

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R-268712, CAS 879487-87-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 44.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 168.00
25 mg	In stock	$ 347.00
50 mg	In stock	$ 588.00
100 mg	In stock	$ 838.00
1 mL * 10 mM (in DMSO)	In stock	$ 116.00

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Purity: 99.77%

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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

Solubility Information

DMSO: 110 mg/mL (302.7 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library TGF-beta/Smad Compound Library Kinase Inhibitor Library Anti-Colorectal Cancer Compound Library Anti-Lung Cancer Compound Library Angiogenesis related Compound Library Cytokine Inhibitor Library Anti-Cancer Compound Library Anti-Obesity Compound Library

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Keywords

R-268712 879487-87-3 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad renal fibrosis Thy1 nephritis Transforming growth factor beta receptors glomerulonephritis Transforming growth factor beta ALK tyrosine kinase receptor HFL-1 glomerulosclerosis CD246 Inhibitor Cluster of differentiation 246 R 268712 UUO Anaplastic lymphoma kinase (ALK) inhibit TGF-β R268712 CKD TGF-β Receptor Anaplastic lymphoma kinase inhibitor

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