Crinecerfont 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. 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.
For research use only. We do not sell to patients.
- CAS No.: 2649012-17-7
- Formula: C34H36ClFN2O4S2
- Molecular Weight:655.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cByJ mice (male, 3-4 months old)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 5 weeks
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Result:Showed no effects on fecal corticosterone metabolite circadian activity; showed no effects on plasma corticosterone levels; showed no effects on HPA axis negative feedback sensitivity.
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Animal Model:BALB/cByJ mice (male, 3-4 months old, chronic stress induced via unpredictable chronic mild stress for 7 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 5 weeks
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Result:Exacerbated fecal corticosterone metabolite concentrations at six out of nine circadian time points; increased basal plasma corticosterone levels; restored corticosterone suppression in the dexamethasone suppression test to improve HPA axis negative feedback sensitivity.
Chemical Information
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CAS No. 2649012-17-7
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Molecular Weight 655.24
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Formula C34H36ClFN2O4S2
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SMILES
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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Synonyms
SSR-125543 tosylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Crinecerfont
- 2649012-17-7
- SSR-125543
- SSR125543
- SSR 125543
- CFTR
- chronic stress conditions
- classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency
- adrenal androgens
- hypothalamic-pituitary-adrenal axis
- depression
- adrenocorticotropic hormone
- corticosterone
- corticotropin-releasing factor receptor type-1
- chronically stressed mice
- anxiety
- Inhibitor
- inhibitor
- inhibit