1. GPCR/G Protein
  2. Vasopressin Receptor
  3. Lixivaptan

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

Cat. No.: HY-14185 Purity: 99.90%
Handling Instructions

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.

For research use only. We do not sell to patients.

Lixivaptan Chemical Structure

Lixivaptan Chemical Structure

CAS No. : 168079-32-1

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10 mM * 1 mL in DMSO USD 88 In-stock
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5 mg USD 84 In-stock
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10 mg USD 144 In-stock
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25 mg USD 312 In-stock
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50 mg USD 552 In-stock
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100 mg USD 984 In-stock
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Based on 1 publication(s) in Google Scholar

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  • References

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Description

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

IC50: 1.2 nM (human V2), 2.3 nM (rat V2)[1]

In Vitro

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

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 Uvol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while Uosm 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].

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

Clinical Trial
Molecular Weight

473.93

Formula

C₂₇H₂₁ClFN₃O₂

CAS No.

168079-32-1

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

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 : ≥ 150 mg/mL (316.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.90%

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LixivaptanVPA-985 WAY-VPA 985VPA985VPA 985Vasopressin ReceptorInhibitorinhibitorinhibit

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