R 268712

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Cat.No. 5288 - R 268712 | C20H18FN5O | CAS No. 879487-87-3
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)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 363.39. Batch specific molecular weights may vary from batch to batch due to solvent 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 5.5 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

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

Terashima et al (2014) R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur.J.Pharmacol. 734 60 PMID: 24726873


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View all TGF-β Receptor Inhibitors

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Citations for R 268712

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Literature in this Area

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Pathways for R 268712

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.