SSR 125543A - SSR 125543 hydrochloride | Crinecerfont hydrochloride

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 1799

CAS [321839-75-2]

MF C27H28ClFN2OS.HCl
MW 519.50

Purity: 98%
Optical purity: Optically pure
Soluble in DMSO

SSR 125543A

Description

Potent, selective, and orally active corticotropin-releasing factor 1 receptor (CRF1) antagonist (pKi values of 8.73 and 9.08 for human cloned or native CRF1 receptors, respectively) with antidepressant-like and anxiolytic-like effects in the Flinders Sensitive Line rats. SSR 125543A shows a 1000-fold selectivity for CRF1 versus CRF2α receptor and CRF binding protein, has a long duration of action, and readily crosses the blood-brain barrier.

A. Urani et al. The corticotropin-releasing factor 1 receptor antagonist, SSR125543, and the vasopressin 1b receptor antagonist, SSR149415, prevent stress-induced cognitive impairment in mice. Pharmacol. Biochem. Behav. 2011, 98, 425-431.

D.H. Overstreet et al. Antidepressant-like effects of CRF1 receptor antagonist SSR125543 in an animal model of depression. Eur. J. Pharmacol. 2004, 497, 49-53.

C.Q. Huang et al. Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists. Bioorg. Med. Chem. Lett. 2004, 14, 2083-2086.

G. Gully et al. 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A).... J. Pharmacol. Exp. Ther. 2002, 301, 322-332.

Potent, selective, and orally active corticotropin-releasing factor 1 receptor (CRF1) antagonist

Chemical name

(S)-4-(2-chloro-4-methoxy-5-methylphenyl)-N-(2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl)-5-methyl-N-(prop-2-ynyl)thiazol-2-amine hydrochloride

Parent CAS No.

[752253-39-7]

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SSR 125543A - SSR 125543 hydrochloride | Crinecerfont hydrochloride

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SSR 125543A - SSR 125543 hydrochloride | Crinecerfont hydrochloride

Description

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