R 268712
Tocris Bioscience, part of Bio-Techne | Catalog # 5288
Potent and selective inhibitor of TGF-βRI
Key Product Details
Description
Potent and selective inhibitor of TGF-βRI
Product Description
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.Product Specifications
Molecular Weight
363.39
Formula
C20H18FN5O
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for R 268712
For research use only
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