d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki 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].
d[Cha4]-AVP binds to hV1b receptors and human oxytocin receptors with pKi 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.
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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.
[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.
d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors[1][2].
d[Cha4]-AVP binds to hV1b receptors and human oxytocin receptors with pKi 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.
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-80deg;C
2 years
-20deg;C
1 year
In solvent
-80deg;C
6 months
-20deg;C
1 month
参考文献
[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.
[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.