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Pexacerfont

Chemical Structure : Pexacerfont

CAS No.: 459856-18-9

Pexacerfont (BMS-562086;BMS562086;DPC-A69448)

Catalog No.: PC-61269Not For Human Use, Lab Use Only.

Pexacerfont (BMS562086, DPC-A69448) is a potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pexacerfont (BMS562086, DPC-A69448) is a potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.
Pexacerfont (BMS562086, DPC-A69448) demonstrates oral effectivity in rat models of anxiety, possesses good pharmacokinetic profile in vivo.

Physicochemical Properties

M.Wt 340.431
Formula C18H24N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine

References

1. Kwako LE, et al. Neuropsychopharmacology. 2015 Mar 13;40(5):1053-63.

2. Gilligan PJ, et al. J Med Chem. 2009 May 14;52(9):3084-92.

3. Schwandt ML, et al. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829.

4. Zhou L, et al. Drug Metab Dispos. 2012 Jun;40(6):1093-103.

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