CP 376395

Product NameCP 376395
CAS175140-00-8
MFC21H30N2O
MW326.48
EINECS
MOL File175140-00-8.mol

Chemical Properties

Melting point	224 °C
Boiling point	434.9±45.0 °C(Predicted)
Density	1.018±0.06 g/cm3(Predicted)
storage temp.	Desiccate at RT
solubility	DMF: 30 mg/ml; DMSO: 15 mg/ml; Ethanol: 30 mg/ml
form	A crystalline solid
pka	7.23±0.48(Predicted)
color	White to off-white

Usage And Synthesis

Uses

CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist[1][2].

Biological Activity

Potent and selective CRF 1 receptor antagonist (K i values are 12 and >10000 nM for CRF 1 and CRF 2 receptors respectively). Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.

in vivo

CP 376395 (10-20 mg/kg, i.p., Male B6 mice) attenuates H2O and food intake, increases sucrose intake, attenuates EtOH intake but not EtOH preference^[2].

Animal Model:	Male B6 mice (n=8-9 per group)^[2]
Dosage:	0.0, 10.0, or 20.0 mg/kg
Administration:	Intraperitoneally
Result:	Dose-dependently attenuated intake of H2O and food, with H2O intake affected specifically during the first half of the session.

IC 50

CRFR1; CRFR2

References

[1] Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92. DOI:10.1021/jm070579c
[2] Giardino WJ, et al. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption. Alcohol Clin Exp Res. 2013 Jul;37(7):1161-70. DOI:10.1111/acer.12076