Pexacerfont
- Product Name
- Pexacerfont
- CAS No.
- 459856-18-9
- Chemical Name
- Pexacerfont
- Synonyms
- BMS-562086;Pexacerfont;Pexacerfont/BMS-562086;Pexacerfont, 10 mM in DMSO;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]-
- CBNumber
- CB22563437
- Molecular Formula
- C18H24N6O
- Formula Weight
- 340.42
- MOL File
- 459856-18-9.mol
Pexacerfont Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 6451
- Product name
- Pexacerfont
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $212
- Updated
- 2021/12/16
- Product number
- CS-6630
- Product name
- Pexacerfont
- Purity
- 99.79%
- Packaging
- 5mg
- Price
- $140
- Updated
- 2021/12/16
- Product number
- CS-6630
- Product name
- Pexacerfont
- Purity
- 99.79%
- Packaging
- 10mg
- Price
- $200
- Updated
- 2021/12/16
- Product number
- CS-6630
- Product name
- Pexacerfont
- Purity
- 99.79%
- Packaging
- 25mg
- Price
- $430
- Updated
- 2021/12/16
- Product number
- CS-6630
- Product name
- Pexacerfont
- Purity
- 99.79%
- Packaging
- 50mg
- Price
- $790
- Updated
- 2021/12/16
Pexacerfont Chemical Properties,Usage,Production
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