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

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.

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Nelivaptan

Nelivaptan Chemical Structure

CAS No. : 439687-69-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Nelivaptan Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Nelivaptan

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

In Vitro

Nelivaptan (0.1-100 nM, 20 min) potently inhibits arginine vasopressin (AVP)-induced Ca2 increase in CHO cells transfected with the human V1b receptor[1].
Nelivaptan (0.9-15 nM, 45 min) inhibits [3H]AVP binding in a competitive manner in CHO cells transfected with the human V1b receptor[1].

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

Nelivaptan Related Antibodies
In Vivo

Nelivaptan (1-30 mg/kg; 30 min i.p. or 2 h p.o. before an exogenous AVP injection) inhibits exogenous AVP-induced increase in plasma corticotropin in Sprague-Dawley rats[1].
Nelivaptan (1-10 mg/kg; p.o.; 1, 2, 3, 4, and 6 h before the AVP challenge) produces powerful dose-dependent inhibition of the corticotropin increase in response to exogenous AVP plus corticotropin-releasing factor (CRF) in Sprague-Dawley rats[1].
Nelivaptan (1-10 mg/kg; i.p. 30 min or 60 min before test; or p.o. for 7 days) displays anxiolytic-like activity after acute and 7-day repeated administrations in male NMRI mice [1].
Nelivaptan (30 mg/kg; i.p.; daily for two weeks) retains efficacy in reducing both measured indices of depression-like behavior (learned helplessness and anhedonia), even when neurogenesis is blocked in male Wistar rats with chronic mild stress[2].

MedChemExpress (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
Molecular Weight

630.11

Formula

C30H32ClN3O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N(C(C=C1)=C2C=C1Cl)C([C@@]2(C3=CC=CC=C3OC)N4[C@@H](C[C@@H](O)C4)C(N(C)C)=O)=O)(C(C(OC)=C5)=CC=C5OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (158.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5870 mL 7.9351 mL 15.8702 mL
5 mM 0.3174 mL 1.5870 mL 3.1740 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

SDS (393 KB)

COA (266 KB) HNMR (309 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5870 mL 7.9351 mL 15.8702 mL 39.6756 mL
5 mM 0.3174 mL 1.5870 mL 3.1740 mL 7.9351 mL
10 mM 0.1587 mL 0.7935 mL 1.5870 mL 3.9676 mL
15 mM 0.1058 mL 0.5290 mL 1.0580 mL 2.6450 mL
20 mM 0.0794 mL 0.3968 mL 0.7935 mL 1.9838 mL
25 mM 0.0635 mL 0.3174 mL 0.6348 mL 1.5870 mL
30 mM 0.0529 mL 0.2645 mL 0.5290 mL 1.3225 mL
40 mM 0.0397 mL 0.1984 mL 0.3968 mL 0.9919 mL
50 mM 0.0317 mL 0.1587 mL 0.3174 mL 0.7935 mL
60 mM 0.0265 mL 0.1323 mL 0.2645 mL 0.6613 mL
80 mM 0.0198 mL 0.0992 mL 0.1984 mL 0.4959 mL
100 mM 0.0159 mL 0.0794 mL 0.1587 mL 0.3968 mL
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Nelivaptan Related Classifications

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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