NBI 35965 methanesulfonate

CAS: 603151-83-3 F: C22H26Cl2N4O3S W: 497.44

NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (

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Bioactivity	NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects[1][2].
Invitro	NBI 35965 methanesulfonate 对 CRF1 表现出高亲和力，但对 CRF2 没有结合亲和力。在 CRF1 转染细胞中，NBI 35965 methanesulfonate 还可抑制 Sauvineine 诱导的 cAMP 刺激[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NBI 35965 methanesulfonate 相关抗体:
In Vivo	NBI 35965 methanesulfonate（20 mg/kg；口服灌胃；一次）可减少小鼠应激诱导的 ACTH 产生[1]。在大鼠中，NBI 35965 methanesulfonate（化合物 12a；10mg/kg）的分布容积为 17.8 L/kg，血浆清除率为 17 mL/min/kg，半衰期为 12 小时。估计口服生物利用度为 34%，1 小时平均最大血浆浓度为 560 ng/mL。NBI 35965 methanesulfonate 也能穿透血脑屏障，导致平均最大脑浓度为 700 ng/g[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	603151-83-3
Formula	C22H26Cl2N4O3S
Molar Mass	497.44
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Gross RS, et al. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J Med Chem. 2005 Sep 8;48(18):5780-93. [2]. Mulugeta Million, et al. A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 2003 Sep 19;985(1):32-42.