R-268712 free base · Synonyms: R 268712 · R268712
R-268712 is an orally active and selective ALK-5 inhibitor.
For research use only. Not for human or veterinary use.
R-268712 structure
CAS No.: 879487-87-3
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 250 mg | USD 420.00 | BP-02096-250mg | In stock | Get quote |
| 500 mg | USD 670.00 | BP-02096-500mg | In stock | Get quote |
| 1 g | USD 1,075.00 | BP-02096-1g | In stock | Get quote |
| 2 g | USD 1,730.00 | BP-02096-2g | In stock | Get quote |
| 3 g | USD 2,065.00 | BP-02096-3g | In stock | Get quote |
| 5 g | USD 2,750.00 | BP-02096-5g | In stock | Get quote |
| 10 g | USD 4,400.00 | BP-02096-10g | In stock | Get quote |
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Description
R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer .
Biological activity
In Vitro R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells[1]. R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells. In Vivo R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC0-24 values of 0.075, 0.28, 1.6 and 8.2 μg h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively. R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model. R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg.
Identifiers
- SMILES
-
CC1=CC=CC(=N1)C1=C(C=NN1)C1=CC(C2=CN(CCO)N=C2)=C(F)C=C1 - InChIKey
-
JQGOCCALXFSRHZ-UHFFFAOYSA-N
Specifications
- MW (average)
- 363.3882
- Formula
- C20H18FN5O
- CAS No.
- 879487-87-3
- Physical state
- Solid
- Color
- White to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO