Home GPCR & G Protein Vasopressin Receptor antagonist Lixivaptan (VPA-985)

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Lixivaptan (VPA-985) Vasopressin Receptor antagonist

Cat.No.S2815

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) Vasopressin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 473.93

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (200.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

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Chemical Information, Storage & Stability

Molecular Weight 473.93 Formula

C27H21ClFN3O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 168079-32-1 -- Storage of Stock Solutions

Synonyms CRTX 080, WAY VPA 985 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

Mechanism of Action

Targets/IC50/Ki
human V2 receptor
1.2 nM
rat V2 receptor
2.3 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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 --

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