d[Cha4]-AVP TFA 

d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a K_i of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors^[1][2].

Ki: 1.2 nM (vasopressin V1B receptor), 151 nM (vasopressin V1A receptor), 240 nM (Oxytocin receptor), 750 nM (vasopressin V2 receptor)

d[Cha4]-AVP binds to hV1b receptors and human oxytocin receptors with pK_i values of 9.68 and 7.68, respectively^[2].
d[Cha4]-AVP stimulates [Ca²⁺]_i increase in hV1b-CHO cells with a pEC₅₀ value of 10.05. d[Cha4]-AVP shows pEC₅₀ values of 6.53 and 5.92 at hV1a and hV2 receptors, respectively, and behaved as a weak antagonist at hOT receptors (pKB=6.31)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

C₅₀H₇₁N₁₃O₁₁S₂

{Mpa}-Tyr-Phe-{Cha}-Asn-Cys-Pro-Arg-Gly-NH2 (Disulfide bridge:Mpa1-Cys6)

{Mpa}YF{Cha}NCPRG-NH2 (Disulfide bridge:Mpa1-Cys6)

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ling Ling Cheng, et al. Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88.  [Content Brief]

  [2]. Cristiana Griffante, et al. Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol. 2005 Nov;146(5):744-51.  [Content Brief]