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Sigma-Aldrich |
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021-61415566 800-8193336 |
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| | CP 376395 Basic information |
| Product Name: | CP 376395 | | Synonyms: | CP 376395;CP 376395 hydrochloride;N-(1-Ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinaminehydrochloride;CP376395;CP-376395;CP 376395;4-Pyridinamine, N-(1-ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-;inhibit,CP376395,Inhibitor,Corticotropin-releasing Factor Receptor,CRFR,CP 376395,CP-376395;2-(Mesityloxy)-3,6-dimethyl-N-(pentan-3-yl)pyridin-4-amine;3,6-dimethyl-N-(pentan-3-yl)-2-(2,4,6-trimethylphenoxy)pyridin-4-amine | | CAS: | 175140-00-8 | | MF: | C21H30N2O | | MW: | 326.48 | | EINECS: | | | Product Categories: | | | Mol File: | 175140-00-8.mol |  |
| | CP 376395 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 |
| | CP 376395 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 |
| | CP 376395 Preparation Products And Raw materials |
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