1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Alvimopan

Alvimopan  (Synonyms: 爱维莫潘; ADL 8-2698; LY 246736)

目录号: HY-13243
产品使用指南

Alvimopan (ADL 8-2698) 是一种有效,选择性,具有口服活性和可逆的 μ-阿片受体 (μ-opioid receptor) 拮抗剂,IC50 值为 1.7 nM。Alvimopan 对 μ-阿片受体 (Ki=0.47 nM) 的选择性高于 κ- (Ki=100 nM) 和 δ-阿片受体 (Ki=12 nM)。Alvimopan 可用于术后肠梗阻的研究。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Alvimopan monohydrate 通常具有更好的水溶性和稳定性。

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Alvimopan Chemical Structure

Alvimopan Chemical Structure

CAS No. : 156053-89-3

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Alvimopan 的其他形式现货产品:

Other Forms of Alvimopan:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus[1][2][3].

IC50 & Target

IC50: 1.7 nM (μ-opioid receptor)[1]

体外研究
(In Vitro)

Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 value of 1.7 nM[1].

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

体内研究
(In Vivo)

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113Sn-labelled microspheres produced by morphine in rats[3].
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[3].

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

Clinical Trial
分子量

424.53

Formula

C25H32N2O4

CAS 号
中文名称

爱维莫潘;阿维莫泮;爱维莫泮

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
  • 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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