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Lixivaptan

Cat. No. M11395
Lixivaptan Structure
Synonym:

VPA-985; WAY-VPA 985

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 155  USD155 In stock
25mg USD 330  USD330 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active, selective vasopressin receptor V2 antagonist with IC50 values of 1.2 nM in humans and 2.3 nM in rats.

Product Citations
Chemical Information
Molecular Weight 473.93
Formula C27H21ClFN3O2
CAS Number 168079-32-1
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Annarita Di Mise, et al. Int J Mol Sci. Lixivaptan, a New Generation Diuretic, Counteracts Vasopressin-Induced Aquaporin-2 Trafficking and Function in Renal Collecting Duct Cells

[2] Mario Rodriguez, et al. Curr Cardiol Rev. Hyponatremia in Heart Failure: Pathogenesis and Management

[3] George Liamis, et al. Expert Rev Clin Pharmacol. Treatment of hyponatremia: the role of lixivaptan

[4] Jalal K Ghali, et al. IDrugs. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia

[5] Elaine Ku, et al. Expert Opin Investig Drugs. Lixivaptan: a novel vasopressin receptor antagonist

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Keywords: Lixivaptan, VPA-985; WAY-VPA 985 supplier, Vasopressin Receptor, inhibitors, activators


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