A CRF1 antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Crinecerfont

Item No. 45039

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-2-propyn-1-yl-2-thiazolamine
CAS Number
752253-39-7
Synonyms
  • NBI 74788
  • SSR 125543
Molecular Formula
C27H28ClFN2OS
Formula Weight
483.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
ClC(C=C(C(C)=C1)OC)=C1C2=C(C)SC(N([C@H](C3=CC(F)=C(C=C3)C)CC4CC4)CC#C)=N2
InChi Code
InChI=1S/C27H28ClFN2OS/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/t24-/m0/s1
InChi Key
IEAKXXNRGSLYTQ-DEOSSOPVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $68

    Add

    5 mg

    $323

    Add

    10 mg

    $612

    Add
    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    Product Description

    Crinecerfont is an antagonist of corticotropin-releasing factor receptor 1 (CRF1; Ki = 1.9 nM).1 It is selective for CRF1 over CRF2α and a panel of 125 receptors, transporters, ion channels, and enzymes at 10 µM. Crinecerfont inhibits CRF-induced cAMP production in Y79 retinoblastoma cells (IC50 = 3 nM) and CRF-induced adrenocorticotropic hormone (ACTH) secretion in AtT-20 mouse pituitary tumor cells when used at concentrations of 3, 30, and 100 nM. In vivo, crinecerfont (10 mg/kg, p.o.) prevents restraint stress-induced increases in plasma ACTH levels in rats. It increases punished responding in the Vogel punished drinking task, indicating anxiolytic-like activity, in mice and decreases immobility time in the forced swim test in rats.2 Crinecerfont (30 mg/kg) decreases cumulative weight gain and increases protein gain in fa/fa obese but not lean rats.3 Formulations containing crinecerfont have been used as an adjunct to glucocorticoids in the treatment of classic congenital adrenal hyperplasia (CAH), an inborn error of metabolism characterized by a deficiency in steroid 21-hydroxylase, also known as cytochrome P450 isoform 21 (CYP21).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gully, D., Geslin, M., Serva, L., 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): A potent and selective corticotrophin-releasing factor1 receptor antagonist. I. Biochemical and pharmacological characterization. J. Pharmacol. Exp. Ther. 301(1), 322-332 (2002).

    2. Griebel, G., Simiand, J., Steinberg, R., 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), a potent and selective corticotrophin-releasing factor1 receptor antagonist. II. Characterization in rodent models of stress-related disorders. J. Pharmacol. Exp. Ther. 301(1), 333-345 (2002).

    3. Doyon, C., Samson, P., Lalonde, J., et al. Effects of the CRF1 receptor antagonist SSR125543 on energy balance and food deprivation-induced neuronal activation in obese Zucker rats. J. Endocrinol. 193(1), 11-19 (2007).