| Name | LIXIVAPTAN |
| Description | Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM) |
| 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]. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.44 mM), Sonication is recommended.
DMSO : 150 mg/mL (316.5 mM), Sonication is recommended.
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| Keywords | WAY-VPA-985 | WAY-VPA985 | VPA985 | VPA 985 | VasopressinReceptor | Vasopressin Receptor | LIXIVAPTAN | Inhibitor | inhibit |
| Inhibitors Related | Mozavaptan | Desmopressin acetate (16679-58-6 free base) | OPC-51803 | Felypressin acetate | Nelivaptan | PF-184563 | Ornipressin Acetate(3397-23-7,free) | d[Leu4,Lys8]-VP acetate | E-4177 | Fuscoside | Tolvaptan | WAY-267464 |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
