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SML4287

Crinecerfont hydrochloride

≥98% (HPLC), powder, CRF1 antagonist

Synonym(s):

(S)-4-(2-Chloro-4-methoxy-5-methylphenyl)-N-(2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl)-5-methyl-N-(prop-2-yn-1-yl)thiazol-2-amine hydrochloride, [4-(2-Chloro-4-methoxy-5-methylphenyl)-5-methylthiazol-2-yl][(1S)-(2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl)]prop-2-ynylamine hydrochloride, SSR 125543A HCl, SSR125543A HCl

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About This Item

Empirical Formula (Hill Notation):
C27H28ClFN2OS·HCl
CAS Number:
321839-75-2
Molecular Weight:
519.50
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Application

Crinecerfont hydrochloride is suitable for use as a CRF-R1 antagonist to study its effects on hypothalamic–pituitary–adrenal (HPA) axis basal circadian activity and negative feedback sensitivity in mice models.

Biochem/physiol Actions

Crinecerfont HCl exhibits nanomolar affinity (Kᵢ ~ 0.8-1.8 nM) for CRF1 receptors across human recombinant (hCRF1-CHO cells, pKᵢ = 8.73) , human native (Y79 cells, pKᵢ = 9.08), rat (pKᵢ = 8.77), mouse (pKᵢ = 8.90), and gerbil (pKᵢ = 9.00) brain tissues, while demonstrating a >1,000-fold selectivity against CRF2a receptors and CRF binding protein. Functionally, Crinecerfont’s mechanism of action is through the CRF1 receptor, modulating the cAMP pathway, and competitively inhibiting CRF-induced cAMP production (IC50 = 3.0 nM) in human retinoblastoma Y79 cells and CRF-stimulated adrenocorticotropic hormone (ACTH) secretion in mouse pituitary AtT-20 cells, without displaying any intrinsic agonist activity, demonstrating a highly selective inhibition of CRF1 receptor function. Furthermore, Crinecerfont also influences the cholinergic and noradrenergic systems, reducing hippocampal acetylcholine release and cortical norepinephrine release in rats under stress conditions.

Disclaimer

Hygroscopic Store with desiccant

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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