R 268712

Name: R 268712
Brand: Tocris Bioscience
SKU: 5288
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 5288

Citations (4)

COA / SDS

Potent and selective inhibitor of TGF-βRI

Key Product Details

Description:	Potent and selective inhibitor of TGF-βRI
Chemical Name:	4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
Purity:	≥98% (HPLC)
Molecular Weight:	363.39

View Full Technical Details for R 268712

Technical Data
Citations

Biological Activity for R 268712

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.

Compound Libraries for R 268712

R 268712 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for R 268712

M. Wt	363.39
Formula	C₂₀H₁₈FN₅O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	879487-87-3
PubChem ID	11703284
InChi Key	JQGOCCALXFSRHZ-UHFFFAOYSA-N
Smiles	OCCN1N=CC(C2=C(F)C=CC(C3=CNN=C3C4=CC=CC(C)=N4)=C2)=C1

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.

Solubility for R 268712

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	36.34	100
	ethanol	18.17	50

Preparing Stock Solutions for R 268712

The following data is based on the product molecular weight 363.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.75 mL	13.76 mL	27.52 mL
5 mM	0.55 mL	2.75 mL	5.50 mL
10 mM	0.28 mL	1.38 mL	2.75 mL
50 mM	0.06 mL	0.28 mL	0.55 mL

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References for R 268712

References are publications that support the biological activity of the product.

Terashima 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 PMID: 24726873