2. GPCR/G Protein
  3. CRFR
  4. NBI 35965 hydrochloride

NBI 35965 hydrochloride 是一种选择性、具有口服活性、可穿过血脑屏障的促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，Ki 值为 4 nM，pKi 值为 8.5，并且不抑制 CRF2。NBI 35965 hydrochloride 可减少体内 CRF 或应激诱导的促肾上腺皮质激素 (ACTH) 的产生，pIC50 值分别为 7.1 和 6.9。NBI 35965 hydrochloride 具有抗焦虑作用。

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NBI 35965 hydrochloride Chemical Structure

NBI 35965 hydrochloride Chemical Structure

CAS No. : 1782228-59-4

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Other Forms of NBI 35965 hydrochloride:

NBI 35965 hydrochloride 相关抗体

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CRFR1 CRFR2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NBI 35965 hydrochloride 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 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects[1][2].

IC50 & Target[1][2]

CRFR1

4 nM (Ki)

CRFR1

8.5 (pKi)

体外研究
(In Vitro)

NBI 35965 hydrochloride 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 hydrochloride 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.

NBI 35965 hydrochloride 相关抗体:
体内研究
(In Vivo)

NBI 35965 hydrochloride（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 hydrochloride（化合物 12a；10 mg/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 hydrochloride 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: Male CD-1 mice (24-26 g) bearing restraint stress[1]
Dosage: 20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water)
Administration: Oral gavage; 60 min prior to the initiation of the stressor
Result: Reduced stress induced ACTH production in vivo.
分子量

437.79

Formula

C21H23Cl3N4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NBI 35965 hydrochloride 相关分类

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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NBI 359651782228-59-4NBI35965NBI-35965CRFRCorticotropin-releasing Factor ReceptorCRHRCRF1 AntagonistACTHorally activebrain-penetrantanxiolytic effectsInhibitorinhibitorinhibit

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NBI 35965 hydrochloride
目录号：
HY-110056
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