| Identification | Back Directory | [Name]
R-268712 | [CAS]
879487-87-3 | [Synonyms]
2025
R-268712
R 268712;R268712
4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]- | [Molecular Formula]
C20H18FN5O | [MDL Number]
MFCD28963939 | [MOL File]
879487-87-3.mol | [Molecular Weight]
363.39 |
| Chemical Properties | Back Directory | [Boiling point ]
576.8±50.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO : 125 mg/mL (343.98 mM) | [form ]
Solid | [pka]
10.96±0.50(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
R 268712 is an orally active transforming growth factor-β type I receptor inhibitor, which prevents glomerular sclerosis in a Thy1 nephritis model. | [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[2].
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[2].
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[2]. | Animal Model: | Male WKY/Hos rats[2]. | | Dosage: | 0.3, 1, 3, and 10 mg/kg | | Administration: | Oral administration; single. | | Result: | 1.19Pharmacokinetic Parameters of R-268712 in male WKY/Hos rats (n=4)[2].
| PO (0.3 mg/kg) | PO (1 mg/kg) | PO (3 mg/kg) | PO (10 mg/kg) | | AUC0-24 (μg?h/mL) | 0.075 | 0.28 | 1.6 | 8.2 |
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| Animal Model: | Male Col1a1-Luc Tg rats (10 to14-week-old; UUO model; n=5-6)[2]. | | Dosage: | 1, 3, 10 mg/kg | | Administration: | Oral administration; single daily for 3 days. | | Result: | Suppressed activity of renal luciferase in a dose-dependent manner. |
| Animal Model: | Male WKY/Hos rats (4-week-old; Thy1 nephritis model; n=7)[2]. | | Dosage: | 0.3, 1 mg/kg | | Administration: | Oral administration; single daily for 33 days. | | Result: | Significantly reduced proteinuria at day 21( the repression continued until day 28), and serum creatinine level (dosage at 1 mg/kg).
Apparently suppressed glomerular sclerosis by 28% and reduced the increase of the hydroxyproline content when at 1 mg/kg.
Suppressed the activation of mesangial parenchymal cell and the injury of podocyte on the basis of TGF-β signaling inhibition at 1 mg/kg.
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| [IC 50]
TGFBR1: 2.5 nM (IC50); Smad3: 10.4 nM (IC50) | [storage]
Store at -20°C |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|