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SSR 125543A
- SSR 125543 hydrochloride - Crinecerfont hydrochloride
Axon 1799
- Parent CAS: 752253-39-7
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C27H28ClFN2OS.HCl
- MW: 519.5
Description
SSR 125543A (Crinecerfont) is a potent, selective and orally active corticotropin-releasing factor 1 receptor (CRF1/CRHR1) antagonist with reported pKi values of 8.73 and 9.08 at cloned and native human CRF1 receptors.
CRF1 signaling is a central regulator of stress responsivity, hypothalamic-pituitary-adrenal axis activation and anxiety-related neuroendocrine pathways. SSR 125543A is used to study CRF1 receptor pharmacology and stress-linked CNS biology.
Key Features
- Potent CRF1 receptor antagonist
- Reported pKi values: 8.73 and 9.08 at human CRF1 receptors
- Orally active and selective CRF1 pharmacology tool
- Relevant to stress, anxiety and HPA-axis signaling research
Applications
- CRF1 receptor binding and functional assays
- Stress neurobiology and HPA-axis studies
- Anxiety and depression-related pharmacology models
- Neuroendocrine signaling research
More Information
| Parent CAS No. | 752253-39-7 |
|---|---|
| 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 |
| SMILES | S1C(C)=C(C2=CC(C)=C(OC)C=C2Cl)N=C1N([C@H](C1=CC=C(C)C(F)=C1)CC1CC1)CC#C.Cl |&1:17,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H28ClFN2OS.ClH/c1-6-11-31(24(13-19-8-9-19)20-10-7-16(2)23(29)14-20)27-30-26(18(4)33-27)21-12-17(3)25(32-5)15-22(21)28;/h1,7,10,12,14-15,19,24H,8-9,11,13H2,2-5H3;1H/t24-;/m0./s1 |
| InChiKey | BMXALUHUEGRRCH-JIDHJSLPSA-N |
| CID | 9806689 |
| Short Description | CRF1 antagonist |
References
- 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.
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