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LIXIVAPTAN

Catalog No. T7303 CAS 168079-32-1

Synonyms: WAY-VPA 985, VPA-985

Lixivaptan is an orally active and selective <a href="/target/Vasopressin_Receptor" style="display: inline; color: #c13a36">Vasopressin Receptor</a> V2 antagonist(Ki = 2.3 nM)

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

LIXIVAPTAN, CAS 168079-32-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 54.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 131.00
25 mg	In stock	$ 262.00
50 mg	In stock	$ 446.00
100 mg	In stock	$ 759.00
1 mL * 10 mM (in DMSO)	In stock	$ 86.00

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Purity: 99.33%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lixivaptan 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	WAY-VPA 985, 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 2 years

Solubility Information

DMSO: 150 mg/mL (316.50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Bioactive Compound Library Human Metabolite Library Inhibitor Library Neuronal Signaling Compound Library Clinical Compound Library Preclinical Compound Library Bioactive Compounds Library Max ReFRAME Related Library NO PAINS Compound Library Drug Repurposing Compound Library

Related Products

Related compounds with same targets

d[Leu4,Lys8]-VP acetate Argipressin LIXIVAPTAN Mozavaptan Desmopressin acetate (16679-58-6 free base) Desmopressin Atosiban Fuscoside

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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