1. GPCR/G Protein
  2. Vasopressin Receptor

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

Cat. No.: HY-14185 Purity: 99.57%
Data Sheet SDS 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.

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Lixivaptan Chemical Structure

Lixivaptan Chemical Structure

CAS No. : 168079-32-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $73 In-stock
2 mg $50 In-stock
5 mg $70 In-stock
10 mg $120 In-stock
25 mg $260 In-stock
50 mg $460 In-stock
100 mg $820 In-stock
200 mg   Get quote  
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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].

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].

References
Molecular Weight

473.93

Formula

C₂₇H₂₁ClFN₃O₂

CAS No.

168079-32-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥150 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Lixivaptan
Cat. No.:
HY-14185
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