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MedChemExpress - Model Antalarmin ...

MedChemExpress - Model Antalarmin hydrochloride - 220953-69-5

Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome[1][2][3].

Antalarmin hydrochloride

MCE China：Antalarmin hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-103377

CAS：220953-69-5

Purity：99.87%

Storage：-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome.

In Vitro：Antalarmin (1 µM, 10 minutes) blocks CRH-induced cAMP increase and VEGF production in human mast cells (HMC-1 and hCBMC cells) via CRH-R1[4].

In Vivo：Antalarmin hydrochloride (5, 10, 20 mg/kg, i.p., single dose) blocks CRF-induced anxiety-like behavior and reduces defensive withdrawal in rats[2].

References：

[1]. Webster EL, et al. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology. 1996 Dec;137(12):5747-50. doi: 10.1210/endo.137.12.8940412. [Content Brief]

[2]. Zorrilla EP, et al. Effects of antalarmin, a CRF type 1 receptor antagonist, on anxiety-like behavior and motor activation in the rat. Brain Res. 2002 Oct 18;952(2):188-99. [Content Brief]

[3]. Deak T, et al. The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress. Endocrinology. 1999 Jan;140(1):79-86. [Content Brief]

[4]. Cao J, et al. Human mast cells express corticotropin-releasing hormone (CRH) receptors and CRH leads to selective secretion of vascular endothelial growth factor. J Immunol. 2005 Jun 15;174(12):7665-75. [Content Brief]

Brand introduction:
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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