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Nelivaptan

Name: Nelivaptan
Brand: TargetMol
SKU: T28153
Price: 71 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T28153Cas No. 439687-69-1

Alias SSR149415, SR-149415, SR 149415

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.

Nelivaptan

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Purity: 99.89%

Catalog No. T28153Alias SSR149415, SR-149415, SR 149415Cas No. 439687-69-1

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$71	In Stock	In Stock
5 mg	$153	In Stock	In Stock
10 mg	$220	In Stock	In Stock
25 mg	$367	In Stock	In Stock
50 mg	$545	In Stock	In Stock
100 mg	$785	In Stock	In Stock
500 mg	$1,630	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.89%

ee:97.80%

Appearance:Solid

Color:White

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COA HNMR CSFC LCMS

Product Introduction

Nelivaptan AI Summary

Nelivaptan exhibits high affinity for the human and rat vasopressin V1b receptors with Ki values of 0.6 nM and 1.0 nM, respectively. It shows moderate affinity for the human vasopressin V1a receptor with a Ki value of 22.0 nM and lower affinity for the human vasopressin V2 receptor with a Ki value of 325.0 nM. Additionally, it has affinity for the human oxytocin receptor with a Ki value of 19.0 nM. The compound demonstrates antagonist activity at recombinant V1b, V1a, and oxytocin receptors in CHO cells by inhibiting vasopressin-induced calcium release, with varying Ki values of 58.88 nM and 1.514 nM. Biodistribution studies in baboons show low drug uptake in organs such as the liver, heart, spleen, and lung, with high selectivity ratios for vasopressin V1b receptor over V1a, V2, and oxytocin receptors. The compound exhibits a high intrinsic clearance in human and rat liver microsomes, a short terminal half-life, moderate volume of distribution, and rapid clearance in rat plasma. Additionally, it has decent oral bioavailability in rats but limited brain penetration. Nelivaptan also demonstrates antiviral activity against SARS-CoV-2 with an IC50 value greater than 20,000 nM and mixed effects on cell viability in various cell types, influencing growth rates. It modulates protein stability as indicated by thermal shift assays and shows bioactivity in multiple GPCR beta-arrestin recruitment assays, suggesting complex pharmacological interactions..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.
In vitro	METHODS: Nelivaptan (SR 149415) (1.25 nM, 2.5 nM and 5 nM) was used to treat In-R1-G9 pancreatic model cells, and the inhibitory effect of Nelivaptan on the specific binding of [3H]AVP (radiolabeled vasopressin) was detected. RESULTS As the concentration of Nelivaptan5 increased, the Kd value (dissociation constant) under control conditions showed a dose-dependent decrease, which indicated that Nelivaptan inhibited the binding of [3H]AVP in a competitive manner, and the Ki value of Nelivaptan (inhibition constant) is 1.61 ± 0.17 nM. [1]
In vivo	METHODS: Animals in the male Wistar rat administration group and the Nelivaptan (SR 149415) group were intraperitoneally injected with drug (1ml/kg, 5% DMSO, 95% normal saline) or Nelivaptan dissolved in the drug (1ml/kg; stock solution concentration 5mg/kg) , the rats were placed in a high temperature environment of 38°C for 60 minutes, and the body weight and rectal temperature were measured before and immediately after treatment. RESULTS Nelivaptan treatment reduced intracranial V1bR levels. [2] METHODS: Nelivaptan was injected with DMSO as solvent at a dose of 1 nmol/rat (icv) with a volume of 5µl. The rats were monitored under basal non-stress (NS) conditions, acute stress (AS), CHS and CHeS. Changes in hypothalamic OXT and AVP release under conditions. RESULTS Nelivaptan could eliminate CHS-induced GE damage. [3]
Synonyms	SSR149415, SR-149415, SR 149415

Chemical Properties

Molecular Weight	630.11
Formula	C₃₀H₃₂ClN₃O₈S
Cas No.	439687-69-1
Smiles	O=C1[C@](C=2C(N1S(=O)(=O)C3=C(OC)C=C(OC)C=C3)=CC=C(Cl)C2)(N4[C@H](C(N(C)C)=O)C[C@@H](O)C4)C5=C(OC)C=CC=C5
Relative Density.	1.414 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (396.76 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5870 mL	7.9351 mL	15.8702 mL	79.3512 mL
5 mM	0.3174 mL	1.5870 mL	3.1740 mL	15.8702 mL
10 mM	0.1587 mL	0.7935 mL	1.5870 mL	7.9351 mL
20 mM	0.0794 mL	0.3968 mL	0.7935 mL	3.9676 mL
50 mM	0.0317 mL	0.1587 mL	0.3174 mL	1.5870 mL
100 mM	0.0159 mL	0.0794 mL	0.1587 mL	0.7935 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc