Name: Lixivaptan (VPA-985)
Brand: Selleck Chemicals
SKU: S2815
Rating: 5 (1 reviews)

Lixivaptan (VPA-985, CRTX 080, WAY VPA 985) is an oral, non-peptide, selective V2 receptor vasopressin antagonist with IC50s of 1.2 nM and 2.3 nM for human V2 receptor and rat V2 receptor, respectively.

Lixivaptan (VPA-985) Chemical Structure

CAS: 168079-32-1

Purity & Quality Control

Batch: S281501 DMSO] 95 mg/mL] false] Ethanol] 7 mg/mL] false] Water] Insoluble] false Purity: 99.48%

99.48

Lixivaptan (VPA-985) Related Products

Related Targets	Vasopressin receptor 1 Vasopressin receptor 2	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ GPCR Compound Library	Click to Expand

Signaling Pathway

Vasopressin Receptor Signaling Pathway

Choose Selective Vasopressin Receptor Inhibitors

Biological Activity

Description

Lixivaptan (VPA-985, CRTX 080, WAY VPA 985) is an oral, non-peptide, selective V2 receptor vasopressin antagonist with IC50s of 1.2 nM and 2.3 nM for human V2 receptor and rat V2 receptor, respectively.

Targets

human V2 receptor ^[1]	rat V2 receptor ^[1]
1.2 nM	2.3 nM

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05208866	Terminated	Polycystic Kidney Disease Adult	Palladio Biosciences\|Centessa Pharmaceuticals plc	February 10 2022	Phase 3
NCT04064346	Terminated	Autosomal Dominant Polycystic Kidney\|ADPKD	Palladio Biosciences\|Centessa Pharmaceuticals plc	October 28 2021	Phase 3
NCT04152837	Terminated	Polycystic Kidney Disease Adult\|ADPKD	Palladio Biosciences\|Centessa Pharmaceuticals plc	September 2 2020	Phase 3
NCT03487913	Completed	Autosomal Dominant Polycystic Kidney Disease	Palladio Biosciences	September 14 2018	Phase 2
NCT01055912	Completed	Congestive Heart Failure	CardioKine Inc.\|Cardiokine Biopharma LLC	January 2010	Phase 2
NCT01056848	Completed	Hyponatremia With Normal Extracellular Fluid Volume\|Hyponatremia With Excess Extracellular Fluid Volume	CardioKine Inc.\|Cardiokine Biopharma LLC\|Biogen	January 2010	--

References

Chemical Information & Solubility

Molecular Weight	473.93	Formula	C₂₇H₂₁ClFN₃O₂
CAS No.	168079-32-1	SDF	--
Smiles	CC1=C(C=C(F)C=C1)C(=O)NC2=CC(=C(C=C2)C(=O)N3CC4=CC=C[N]4CC5=CC=CC=C35)Cl
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 95 mg/mL ( (200.45 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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