2. GPCR/G Protein
  3. Vasopressin Receptor
  4. V1a/V2 antagonist 1

V1a/V2 antagonist 1 (Compound 18j) 是一种具有口服活性的双靶点的 V1a 和 V2 拮抗剂，对 V1a 和 V2 受体均具有很强的结合亲和力 (Ki: hV1a 为 0.13 nM, hV2 为 0.53 nM, mV1a 为 0.5 nM; IC50: hV1a为 2.2 nM )。V1a/V2 antagonist 1 可抑制 Oxytocin (HY-17571) 诱发的小鼠抓挠行为。

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V1a/V2 antagonist 1 Chemical Structure

V1a/V2 antagonist 1 Chemical Structure

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V1a/V2 antagonist 1 相关抗体

Top Publications Citing Use of Products

查看 Vasopressin Receptor 亚型特异性产品:

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V1a Receptor  V1b Receptor  V2 Receptor 

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice[1].

IC50 & Target[1]

human V1a Receptor

0.13 nM (Ki)

human V2 Receptor

0.53 nM (Ki)

human V1a Receptor

2.2 nM (IC50)

体外研究
(In Vitro)

V1a/V2 antagonist 1 (1 μM) 具有良好的的肝微粒体代谢稳定性，其 Clint (h/r/m) (μL/min/mg) 为15.9/36.9/ 27.1[1]。
V1a/V2 antagonist 1 与 hERG 没有相互作用 (IC50：>30 μM)，PDR 值为 0.91 (VB-Caco-2 渗透性试验) [1]。

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

V1a/V2 antagonist 1 相关抗体:
体内研究
(In Vivo)

V1a/V2 antagonist 1 (0.1-3 mg/kg，口服，60 min 预处理) 显著抑制 Oxytocin (HY-17571) 诱发的小鼠抓挠行为[1]。

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

Animal Model: OT-induced scratching in mice [1]
Dosage: 0.1, 0.3, 1, 3 mg/kg
Administration: Oral gavage (p.o.), 60-min pretreatment
Result: Inhibited scratching with inhibition rate of 86% (3 mg/kg), 91% (1 mg/kg), 85% (0.3 mg/kg) and 81% (0.1 mg/kg).
分子量

479.96

Formula

C25H26ClN5O3
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

V1a/V2 antagonist 1 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.

Keywords:

V1a/V2 antagonist 1Vasopressin ReceptorScratchingGroomingPermeabilityMicrosomalVB-Caco-2CHO cellsInhibitorinhibitorinhibit

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产品名称：
V1a/V2 antagonist 1
目录号：
HY-168742
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