2. GPCR/G Protein
  3. Vasopressin Receptor
  4. Nelivaptan

Nelivaptan  (Synonyms: SSR-149415)

目录号: HY-10066 纯度: 99.89%
COA 产品使用指南 技术支持

Nelivaptan (SSR-149415) 是一种具有口服活性的选择性 vasopressin V1b Receptor 拮抗剂 (对天然和重组大鼠 V1b 受体的 Ki 值分别为 3.7 和 1.3 nM)。Nelivaptan 抑制精氨酸加压素 (AVP) 诱导的 Ca2+ 增加和促肾上腺皮质激素分泌。Nelivaptan 可用于压力、焦虑及抑郁症的研究。

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Nelivaptan

Nelivaptan Chemical Structure

CAS No. : 439687-69-1

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1 mg ￥720
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5 mg ￥1480
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10 mg ￥2200
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Nelivaptan 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

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression[1][2].

体外研究
(In Vitro)

Nelivaptan (0.1-100 nM，20 分钟) 在转染了人 V1b 受体的 CHO 细胞中有效抑制精氨酸加压素 (AVP) 诱导的 Ca2 增加[1]。
Nelivaptan (0.9-15 nM，45 分钟) 在转染了人 V1b 受体的 CHO 细胞中以竞争性方式抑制 [3H]AVP 结合[1]。

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

Nelivaptan 相关抗体:
体内研究
(In Vivo)

Nelivaptan (1-30 mg/kg；注射外源性 AVP 前 30 分钟腹腔注射或 2 小时口服) 可抑制 Sprague-Dawley 大鼠中外源性 AVP 诱导的血浆促皮质素增加[1]。
Nelivaptan (1-10 mg/kg；口服；注射 AVP 前 1、2、3、4 和 6 小时) 在 Sprague-Dawley 大鼠中剂量依赖性抑制由外源性 AVP 加促肾上腺皮质激素释放因子刺激引起的促肾上腺皮质激素增加[1]。
Nelivaptan (1-10 mg/kg；测试前 30 分钟或 60 分钟腹腔注射；或口服 7 天) 在雄性 NMRI 小鼠中，急性和 7 天重复给药后表现出抗焦虑样活性[1]。
Nelivaptan (30 mg/kg；腹腔注射；每天给药，连续两周) 在慢性轻度应激的雄性 Wistar 大鼠中，即使在神经发生受阻的情况下，仍能有效降低抑郁样行为的测量指标 (习得性无助和快感缺乏) [2]。

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

Animal Model: Male Wistar rats (300-400 g, aged 3 months) with chronic mild stress[2]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.); daily for two weeks
Result: Chronic administration reversed learned helplessness and anhedonia even when methylazoxymethanol (MAM) was administered.
Attenuated these depressive-like behaviors after 1 week.
Restored the density of Ki-67-positive cells to control levels.
Animal Model: Male Sprague-Dawley CD rats (275-300 g)[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: Intraperitoneal injection (i.p.) or Oral gavage (p.o.); 30 min i.p. or 2 h p.o. before an exogenous AVP injection
Result: Antagonized AVP-induced corticotropin secretion in a dose-dependent manner by both intraperitoneal and oral routes.
The inhibition was significant from 10 mg/kg p.o. and 3 mg/kg i.p. upwards.
The inhibitory action lasted significantly for more than 2 h at 10 mg/kg i.p. and up to 4 h at 10 mg/kg p.o..
Had no effect on basal corticotropin plasma levels up to 30 mg/kg p.o..
Animal Model: Male Sprague-Dawley CD rats (275-300 g)[1]
Dosage: 1, 3, 10 mg/kg
Administration: Oral gavage (p.o.); 1, 2, 3, 4, and 6 h before the AVP challenge (10 mg/kg)
Result: Produced powerful dose-dependent inhibition of the corticotropin increase in response to exogenous AVP plus corticoliberin; the effect was significant from the dose of 3 mg/kg p.o.. Complete blockade was achieved at 10 mg/kg.
Showed a fast onset of action, the inhibitory effect was maximal at 1 h after administration.
The inhibitory effect on corticotropin secretion lasted significantly more than 4 h, demonstrating a long-lasting oral effect in a specific V1b-related model.
Animal Model: Male NMRI mice (20 g)[1]
Dosage: 1, 3, 10 mg/kg
Administration: Intraperitoneal injection (i.p.) or Oral gavage (p.o.); i.p. (1, 3, 10 mg/kg) 30 min or 60 min befeore; p.o. (10 mg/kg) for 7 days,
Result: In the acute experiments, i.p. and p.o. compound increased the number of punished crossings showing marked anxiolytic effects.
Post hoc analysis revealed that these effects reached statistical significance from 3 mg/kg p.o. and i.p.
The anxiolytic-like activity was still significantly maintained when given repeatedly at 10 mg/kg p.o. for 7 days.
The oral time course of the anxiolytic-like action performed at 10 mg/kg indicated that effects lasted for more than 4 h.
Clinical Trial
分子量

630.11

Formula

C30H32ClN3O8S
CAS 号
性状

固体

颜色

White to off-white

运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 2 mg/mL (3.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5870 mL 7.9351 mL 15.8702 mL
5 mM --- --- ---
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.89%

COA (303 KB) HNMR (309 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

Nelivaptan 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5870 mL 7.9351 mL 15.8702 mL 39.6756 mL
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:

Nelivaptan439687-69-1SSR-149415SSR149415SSR 149415Vasopressin ReceptorcorticotropinstressanxietyCa2+arginine vasopressindepressionInhibitorinhibitorinhibit

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