Crinecerfont tosylate  (Synonyms: SSR-125543 tosylate)

Crinecerfont (SSR-125543) tosylate is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont tosylate blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont tosylate improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont tosylate can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency^[1][2]. Crinecerfont tosylate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Crinecerfont (SSR-125543) (20 mg/kg; i.p.; daily; 5 weeks) tosylate improves hypothalamic-pituitary-adrenal (HPA) axis negative feedback sensitivity in chronically stressed mice but exacerbates their basal circadian corticosterone secretion, and does not alter HPA axis circadian activity or negative feedback sensitivity in non-stressed control mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

655.24

C₃₄H₃₆ClFN₂O₄S₂

2649012-17-7

C#CCN(C1=NC(C2=C(C=C(C(C)=C2)OC)Cl)=C(S1)C)[C@H](C3=CC(F)=C(C=C3)C)CC4CC4.O=S(C5=CC=C(C)C=C5)(O)=O

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• [1]. Ibarguen-Vargas Y, et al. CRF-R1 Antagonist Treatment Exacerbates Circadian Corticosterone Secretion under Chronic Stress, but Preserves HPA Feedback Sensitivity. Pharmaceutics. 2021;13(12):2114. Published 2021 Dec 8.  [Content Brief]

  [2]. Newfield RS, et al. Crinecerfont, a CRF1 Receptor Antagonist, Lowers Adrenal Androgens in Adolescents With Congenital Adrenal Hyperplasia. J Clin Endocrinol Metab. 2023;108(11):2871-2878.  [Content Brief]