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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
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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
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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.

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N-Bromosuccinimide Price

Tocris
Product number
6451
Product name
Pexacerfont
Purity
≥98%(HPLC)
Packaging
10
Price
$212
Updated
2021/12/16
ChemScene
Product number
CS-6630
Product name
Pexacerfont
Purity
99.79%
Packaging
5mg
Price
$140
Updated
2021/12/16
ChemScene
Product number
CS-6630
Product name
Pexacerfont
Purity
99.79%
Packaging
10mg
Price
$200
Updated
2021/12/16
ChemScene
Product number
CS-6630
Product name
Pexacerfont
Purity
99.79%
Packaging
25mg
Price
$430
Updated
2021/12/16
ChemScene
Product number
CS-6630
Product name
Pexacerfont
Purity
99.79%
Packaging
50mg
Price
$790
Updated
2021/12/16
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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

Pexacerfont Preparation Products And Raw materials

Raw materials

Preparation Products

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Pexacerfont Suppliers

Shanghai Fuhe Chemistry Technology Co., Ltd.
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0086-21-67651705
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China
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LETOPHARM LIMITED
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021-52996696,15000506266 15000506266
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+86-21-52996696
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Amatek Scientific Co. Ltd.
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0512-56316828
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0512-56316826
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Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
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liming@bio-fount.com
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China
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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InvivoChem
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Baimei Jihua (Henan) Pharmaceutical Technology Co., Ltd
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037188900765 18037465274
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Wuhan Topule
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459856-18-9, PexacerfontRelated Search:


  • Pexacerfont
  • Pexacerfont/BMS-562086
  • 8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
  • 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
  • Pyrazolo[1,5-a]-1,3,5-triazin-4-amine, 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]-
  • Pexacerfont, 10 mM in DMSO
  • 459856-18-9