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LIXIVAPTAN

Catalog No. T7303   CAS 168079-32-1
Synonyms: VPA-985, WAY-VPA 985

Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)

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LIXIVAPTAN Chemical Structure
LIXIVAPTAN, CAS 168079-32-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 36.00
2 mg In stock $ 52.00
5 mg In stock $ 74.00
10 mg In stock $ 129.00
25 mg In stock $ 262.00
50 mg In stock $ 446.00
100 mg In stock $ 657.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.33%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)
Targets&IC50 rat V2:2.3 nM (IC50), human V2:1.2 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[1].
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[1].
Synonyms VPA-985, WAY-VPA 985
Molecular Weight 473.93
Formula C27H21ClFN3O2
CAS No. 168079-32-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (316.50 mM)

TargetMolReferences and Literature

1. Wang X, Constans MM, Chebib FT.et al.Effect of a Vasopressin V2 Receptor Antagonist on Polycystic Kidney Disease Development in a Rat Model[J].Am J Nephrol. 2019;49(6):487-493. 2. Di Mise A, Venneri M, Ranieri M.et al.Lixivaptan, a New Generation Diuretic, Counteracts Vasopressin-Induced Aquaporin-2 Trafficking and Function in Renal Collecting Duct Cells.Int J Mol Sci. 2019 Dec 26;21(1).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Clinical Compound Library Preclinical Compound Library Orally Active Compound Library Human Metabolite Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets
(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin Conopressin S acetate(111317-90-9 free base) Felypressin acetate Argipressin Vasopressin Dimer (parallel) (TFA) Dp[Tyr(methyl)2,Arg8]-Vasopressin Val9-Oxytocin (D-Arg8)-Inotocin

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Keywords

LIXIVAPTAN 168079-32-1 GPCR/G Protein Vasopressin Receptor VPA-985 inhibit Inhibitor VPA 985 VPA985 WAY-VPA 985 WAY-VPA-985 WAY-VPA985 inhibitor

 

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