Crinecerfont hydrochloride，5MG，SML4287-5MG，Sigma

销售价： ¥ 1438.82 / 件

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订货号： 0BN2349

品牌型号： Sigma SML4287-5MG

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最小订货量： 1件

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产品介绍 Product Description

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.