Lixivaptan (CAS 168079-32-1)
Alternate Names:
N-[3-Chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methyl-benzamide
CAS Number:
168079-32-1
Molecular Weight:
473.93
Molecular Formula:
C27H21ClFN3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Lixivaptan is a selective, active vasopressin V2 receptor antagonist. It functions by blocking the vasopressin V2 receptors in the renal collecting duct, which inhibits the action of vasopressin on the V2 receptors. This results in a decrease in water reabsorption, leading to increased urine output and a reduction in extracellular fluid volume. At the molecular level, Lixivaptan competes with vasopressin for binding to the V2 receptors, preventing the activation of the Gs protein-coupled signaling pathway. This disrupts the normal physiological response to vasopressin, leading to the desired diuretic effect. In experiments, Lixivaptan′s mode of action involves its specific interaction with vasopressin V2 receptors, resulting in altered renal function and fluid balance.
Lixivaptan (CAS 168079-32-1) References
- Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. | Molinari, AJ., et al. 2007. Bioorg Med Chem Lett. 17: 5796-800. PMID: 17855087
- Vasopressin receptor antagonists and their role in clinical medicine. | Narayen, G. and Mandal, SN. 2012. Indian J Endocrinol Metab. 16: 183-91. PMID: 22470853
- Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. | Prakash, C., et al. 2012. Drug Metab Dispos. 40: 1308-20. PMID: 22474055
- Meta-analysis: the safety and efficacy of vaptans (tolvaptan, satavaptan and lixivaptan) in cirrhosis with ascites or hyponatraemia. | Dahl, E., et al. 2012. Aliment Pharmacol Ther. 36: 619-26. PMID: 22908905
- Lixivaptan: a vasopressin receptor antagonist for the treatment of hyponatremia. | Rosner, MH. 2012. Kidney Int. 82: 1154-6. PMID: 23151986
- Lixivaptan - an evidence-based review of its clinical potential in the treatment of hyponatremia. | Bowman, BT. and Rosner, MH. 2013. Core Evid. 8: 47-56. PMID: 23874242
- Urea minimizes brain complications following rapid correction of chronic hyponatremia compared with vasopressin antagonist or hypertonic saline. | Gankam Kengne, F., et al. 2015. Kidney Int. 87: 323-31. PMID: 25100046
- Development and validation of HPLC-MS/MS method for the determination of lixivaptan in mouse plasma and its application in a pharmacokinetic study. | Kadi, AA., et al. 2017. Biomed Chromatogr. 31: PMID: 28493402
- Effect of a Vasopressin V2 Receptor Antagonist on Polycystic Kidney Disease Development in a Rat Model. | Wang, X., et al. 2019. Am J Nephrol. 49: 487-493. PMID: 31117065
- Lixivaptan, a New Generation Diuretic, Counteracts Vasopressin-Induced Aquaporin-2 Trafficking and Function in Renal Collecting Duct Cells. | Di Mise, A., et al. 2019. Int J Mol Sci. 21: PMID: 31888044
- Comparison of the Hepatotoxic Potential of Two Treatments for Autosomal-Dominant Polycystic Kidney DiseaseUsing Quantitative Systems Toxicology Modeling. | Woodhead, JL., et al. 2020. Pharm Res. 37: 24. PMID: 31909447
- Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. | Liu, C., et al. 2020. Eur J Pharmacol. 880: 173157. PMID: 32360346
- Enantioenriched α-Vinyl 1,4-Benzodiazepines and 1,4-Benzoxazepines via Enantioselective Rhodium-Catalyzed Hydrofunctionalizations of Alkynes and Allenes. | Velasco-Rubio, Á., et al. 2021. J Org Chem. 86: 10889-10902. PMID: 34259003
- Pre-clinical evaluation of dual targeting of the GPCRs CaSR and V2R as therapeutic strategy for autosomal dominant polycystic kidney disease. | Di Mise, A., et al. 2021. FASEB J. 35: e21874. PMID: 34486176
- Optical-Controlled Kinetic Switch: Fine-Tuning of the Residence Time of an Antagonist Binding to the Vasopressin V2 Receptor in In Vitro, Ex Vivo, and In Vivo Models of ADPKD. | Gu, X., et al. 2023. J Med Chem. 66: 1454-1466. PMID: 36563185
Inhibitor of:
AVP, AVP Receptor V2, V1RA3, V1RA4, and V1RI1.Activator of:
AVP Receptor V2, AVP Receptor V3, and V2R.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Lixivaptan, 5 mg | sc-489378 | 5 mg | $84.00 |