Art. -Nr.: HY-14185

Lixivaptan

(Synonyms: VPA-985; WAY-VPA 985)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC₅₀ values of 1.2 and 2.3 nM for human and rat V2, respectively.

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Reinheit: 99.67%
CAS. Nr.: 168079-32-1
Formel: C₂₇H₂₁ClFN₃O₂
Molecular Weight:473.93

Speicherung:

4°C, protect from light

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

Lixivaptan Chemical Structure

CAS. Nr.: 168079-32-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC₅₀ values of 1.2 and 2.3 nM for human and rat V2, respectively.

IC₅₀ & Target

V2 Receptor

Alle Vasopressin Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	124 nM Compound: 2, lixivaptan, CL-347985	Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells	[PMID: 17855087]
CHO	IC₅₀	519 nM Compound: 2, lixivaptan, CL-347985	Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells	[PMID: 17855087]
Fibroblast	IC₅₀	1.2 nM Compound: VPA-985	In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2) In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)	[PMID: 10406632]
Fibroblast	IC₅₀	1.2 nM Compound: 1 (WAY-VPA-985)	Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes	[PMID: 10782686]
Fibroblast	IC₅₀	1.2 nM Compound: 9	Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes	[PMID: 9651149]
HEK293	IC₅₀	150 nM Compound: lixivaptan, VPA-985	Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells	[PMID: 17942308]
HEK293	IC₅₀	5 nM Compound: lixivaptan, VPA-985	Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells	[PMID: 17942308]
HEK293	IC₅₀	91 nM Compound: lixivaptan, VPA-985	Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels	[PMID: 17942308]
HEK293	IC₅₀	>5000 nM Compound: lixivaptan, VPA-985	Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level	[PMID: 17942308]

In Vitro

Lixivaptan displays competitive antagonist activity at V2 receptors^[1].

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

In Vivo

In conscious dogs, water-loaded with 30 mL/kg (po) and arginine vasopressin (AVP)-treated (0.4 μg/kg in oil, sc), lixivaptan (1, 3, and 10 mg/kg po) increases U_vol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while U_osm decreases from 1222 mOsm/kg (water-loaded and AVP treated vehicle) to 307, 221, and 175 mOsm/kg, respectively. In homozygous Brattleboro rats lacking AVP, lixivaptan at 10 mg/kg po (i.e., 10 times the dose producing V2 antagonist activity) b.i.d. for 5 days, shows a sustained antagonist action without evidence of agonist effects. In a randomized double-blind placebo-controlled ascending single dose study, patients (deprived of fluids overnight before dosing) are dosed orally with 30, 75, or 150 mg of lixivaptan. All three doses increase urine flow and serum sodium concentrations and produced significant dose-related decreases in urinary osmolality^[1]. Phase II clinical trials in patients with congestive heart failure, liver cirrhosis with ascites or syndrome of inappropriate antidiuretic hormone have demonstrated that lixivaptan increases water clearance without affecting renal sodium excretion or activating the neurohormonal system^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 168079-32-1
Appearance Solid
Molecular Weight 473.93
Formel C₂₇H₂₁ClFN₃O₂
Color White to off-white
SMILES

O=C(C1=C(Cl)C=C(NC(C2=CC(F)=CC=C2C)=O)C=C1)N(C3)C4=CC=CC=C4CN5C3=CC=C5
Synonyms

VPA-985; WAY-VPA 985
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (4)

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Journal Impact Factor

Eur J Pharmacol

Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. [Abstract]

2020 Aug 5;880:173157. PMID: 32360346
Transl Oncol

HDAC2 promotes malignant progression by the RBM47/NONO axis in medulloblastoma. [Abstract]

2025 Sep 29:62:102549. PMID: 41027284
Continence (Amst)

Endogenous vasopressin and vasopressin receptor 2 in bladder as anti-diuretic / anti-spasmodic targets for the treatment of multifactorial nocturia. [Abstract]

2025 Dec:16:102292. PMID: 41503219
SSRN

2023 May 30.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 150 mg/mL (316.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1100 mL

10.5501 mL

21.1002 mL

5 mM

0.4220 mL

2.1100 mL

4.2200 mL

10 mM

0.2110 mL

1.0550 mL

2.1100 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Albright JD, et al. 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. J Med Chem. 1998 Jul 2;41(14):2442-4. [Content Brief]

[2]. Ghali JK, et al. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia. IDrugs. 2010 Nov;13(11):782-92. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1100 mL	10.5501 mL	21.1002 mL	52.7504 mL
	5 mM	0.4220 mL	2.1100 mL	4.2200 mL	10.5501 mL
	10 mM	0.2110 mL	1.0550 mL	2.1100 mL	5.2750 mL
	15 mM	0.1407 mL	0.7033 mL	1.4067 mL	3.5167 mL
	20 mM	0.1055 mL	0.5275 mL	1.0550 mL	2.6375 mL
	25 mM	0.0844 mL	0.4220 mL	0.8440 mL	2.1100 mL
	30 mM	0.0703 mL	0.3517 mL	0.7033 mL	1.7583 mL
	40 mM	0.0528 mL	0.2638 mL	0.5275 mL	1.3188 mL
	50 mM	0.0422 mL	0.2110 mL	0.4220 mL	1.0550 mL
	60 mM	0.0352 mL	0.1758 mL	0.3517 mL	0.8792 mL
	80 mM	0.0264 mL	0.1319 mL	0.2638 mL	0.6594 mL
	100 mM	0.0211 mL	0.1055 mL	0.2110 mL	0.5275 mL

Keywords

Lixivaptan

4 Cited Publications

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Lixivaptan

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Publications Citing Use of MedChemExpress (MCE) Lixivaptan

Alle Vasopressin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lixivaptan

GPCR/G Protein Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Endocrinology Compound Library

Orally Active Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Human Metabolite Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Lixivaptan

Alle Vasopressin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lixivaptan Related Classifications

HY-14185 Related Classifications