1. GPCR/G Protein
  2. CRFR
  3. NBI-34041

NBI-34041  (Synonyms: SB-723620)

目录号: HY-14128
产品使用指南

NBI-34041 (SB-723620) 是一种选择性口服非肽 CRF1 受体拮抗剂,对人类 CRF1 受体的 IC50 为 58.9 nM,Ki 为 4.0 nM。NBI-34041 对 CRF2 受体没有抑制作用。NBI-34041 可用于抑郁症和焦虑症研究。

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NBI-34041 Chemical Structure

NBI-34041 Chemical Structure

CAS No. : 268545-87-5

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查看 CRFR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

IC50 & Target[1]

CRFR1

58.9 nM (IC50)

CRFR1

4 nM (Ki)

CRFR2

>10000 nM (IC50)

体外研究
(In Vitro)

NBI-34041 可以以浓度依赖性方式抑制 cAMP 的产生,IC50 约为 60 nM。当 NBI-34041 浓度高达 10 000 nM 时,NBI-34041 无法完全抑制表达人类 CRF2 受体的细胞中 sauvagine 刺激的 cAMP[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NBI-34041(3-30 mg/kg;口服管饲;单剂量)可显著减轻 CRF 引起的血浆 ACTH 升高。NBI-34041 还显示出以剂量依赖性方式减轻休克引起的 ACTH 释放的功效[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar or Sprague-Dawley rats (300-350 g)[1]
Dosage: 3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration: Oral gavage; a single dose
Result: Did not impair diurnal adrenocorticotropic hormone (ACTH) and cortisol secretion or CRF evoked ACTH and cortisol responses but attenuated the neuroendocrine response to psychosocial stress.
分子量

417.37

Formula

C22H26Cl2N4

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-34041 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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NBI-34041
目录号:
HY-14128
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