R 268712

Tocris Bioscience | Catalog # 5288

Potent and selective inhibitor of TGF-βRI
Tocris Bioscience

Key Product Details

Description

Potent and selective inhibitor of TGF-βRI
View all TGF-beta Receptor Inhibitors »

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 for R 268712

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.

Select a batch to recalculate based on the batch molecular weight:

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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Background References

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

Product Documents for R 268712

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for R 268712

For research use only

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  • Inhibition of pSmad 2/3 in a human epithelial cell line
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Cell Line/Tissue: A549
    Verified Customer | Posted 10/26/2020
    Tested a human lung epithelial cell line pretreated with R268712 at either 10, 1 or 0.1uM for 30 min and then added TGFb1 at 5ng/ml in two different matrices. Incubated 24hr and then lysed cells to look at pSmad 2/3 levels by immunoassay
    R 268712 5288

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