LIXIVAPTAN

SKU: orb1299938

Description

Lixivaptan (VPA-985) is a potent and selective vasopressin V2 receptor antagonist with a Ki of 2.3 nM. It is an orally bioavailable research tool used in vitro and in vivo to study mechanisms of aquaresis and conditions like hyponatremia and heart failure.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 168079-32-1
• MW: 473.93
• Purity: 98.36%
• Formula: C₂₇H₂₁ClFN₃O₂
• SMILES: Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc23)c(Cl)c1
• Target: Vasopressin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.44 mM);DMSO:150 mg/mL (316.5 mM)

Bioactivity

• Target IC50:
  V2 receptor (rat):2.3 nM (IC50)|V2 receptor (human):1.2 nM (IC50)
• In Vivo:
  Consistent with the development of a polycystic kidney phenotype, control PCK rats showed enlarged kidneys, extensive cyst formation, and early signs of serum creatinine elevation at 12 weeks of age. Compared to controls, PCK rats treated with low-dose lixivaptan showed a 26% reduction in % kidney weight/body weight (p < 0.01); a 54% reduction in kidney cystic score (p < 0.001), a histomorphometric measure of cystic burden; a 23% reduction in kidney cAMP levels (p < 0.05), a biochemical marker of disease; and a 13% reduction in plasma creatinine (p < 0.001), indicating preserved renal function. These reductions were associated with 3-fold increases in 24-h urine output, demonstrating the potent aquaretic effect of lixivaptan.
• Animal Research:
  Four-week old PCK rats were fed rodent chow with 0.5% lixivaptan (low dose) or 1% lixivaptan (high dose), or chow only (control) for 8 weeks. Urine output was measured at weeks 7 and 10 of age. Animals were killed at 12 weeks of age; kidneys and livers were collected, weighted, and analyzed for cyclic adenosine 3',5'-monophosphate (cAMP) levels and cystic burden and fibrosis; serum creatinine and sodium were measured.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, LIXIVAPTAN, WAY-VPA 985, WAY-VPA985, WAY-VPA-985, VasopressinReceptor, Vasopressin Receptor, VPA 985, VPA985, VPA-985

Compound Identifiers

PubChem CID

172997