V2R antagonist

SI-7269

V2R antagonist, >98% (HPLC)

IUPAC Name : N-(4-(5-(2-(3-Chlorophenoxy)ethyl)-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepine-1-carbonyl)phenyl)-[1,1'-biphenyl]-2-carboxamide

Price And Availability
Pack Size	Price in USD	Add To Shopping Cart	Availability	Shipping Status
5MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
10MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
25MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
50MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026
100MG	Request A Quote		Back Order	Estimated to ship on 04 October 2026

Applications : This is a benzodiazepine‑based vasopressin V2R antagonist identified through structure–kinetic relationship (SKR) optimization. Subtle scaffold modifications produced a markedly prolonged residence time (77 min), a 7.7‑fold increase over tolvaptan, without altering binding affinity. This extended target engagement translated into superior in vivo efficacy in an ADPKD model. It exemplifies a kinetics‑driven V2R antagonist with improved pharmacodynamic performance and represents a promising lead for ADPKD therapy.

References : Cao X. et al.: J. Med. Chem., 66(5), 3621-3634, 2023.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.