| Identification | Back Directory | [Name]
Pexacerfont | [CAS]
459856-18-9 | [Synonyms]
BMS-562086
Pexacerfont
Pexacerfont/BMS-562086
N-[(2R)-butan-2-yl]-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
Pyrazolo[1,5-a]-1,3,5-triazin-4-amine, 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]- | [Molecular Formula]
C18H24N6O | [MDL Number]
MFCD22628864 | [MOL File]
459856-18-9.mol | [Molecular Weight]
340.42 |
| Chemical Properties | Back Directory | [Melting point ]
118℃ | [density ]
1.24 | [storage temp. ]
2-8°C(protect from light) | [solubility ]
DMSO: 30 mg/ml; Ethanol: 30 mg/ml | [form ]
A crystalline solid | [pka]
2.08±0.12(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor. | [Definition]
ChEBI: Pexacerfont is a pyrazolopyridine. | [in vivo]
Pexacerfont (BMS-562086) is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus maze models of anxiety. After the intravenous bolus dose, the plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees. The CLp of Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). Assuming the value of CLp of Pexacerfont approximates the value of CLb in these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLp by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLb is equal to CLp is reasonable at least in rats, where the blood to plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose[1]. | [storage]
Store at -20°C | [References]
[1] Zhou L, et al. In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist. Drug Metab Dispos. 2012 Jun;40(6):1093-103. DOI:10.1124/dmd.111.043596 |
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| Company Name: |
Wuhan Topule
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| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
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