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LIXIVAPTAN

LIXIVAPTAN
Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)
Catalog No. T7303Cas No. 168079-32-1
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Purity:98.36%
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LIXIVAPTAN

Catalog No. T7303Cas No. 168079-32-1
Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$52In Stock
5 mg$74In Stock
10 mg$129In Stock
25 mg$262In Stock
50 mg$446In Stock
100 mg$657In Stock
1 mL x 10 mM (in DMSO)$78In Stock
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Product Introduction

Bioactivity
Description
Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)
Targets&IC50
V2 (human):1.2 nM (IC50), V2 (rat):2.3 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].
AliasVPA-985, WAY-VPA 985
Chemical Properties
Molecular Weight473.93
FormulaC27H21ClFN3O2
Cas No.168079-32-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 150 mg/mL (316.50 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1100 mL10.5501 mL21.1002 mL105.5008 mL
5 mM0.4220 mL2.1100 mL4.2200 mL21.1002 mL
10 mM0.2110 mL1.0550 mL2.1100 mL10.5501 mL
20 mM0.1055 mL0.5275 mL1.0550 mL5.2750 mL
50 mM0.0422 mL0.2110 mL0.4220 mL2.1100 mL
100 mM0.0211 mL0.1055 mL0.2110 mL1.0550 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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