d[Cha4]-AVP TFA

d[Cha4]-AVP TFA;

d[Cha4]-AVP TFA 是一种有效的选择性加压素 (AVP) V1b 受体激动剂,对人 V1b 受体的 Ki 为 1.2 nM。d[Cha4]-AVP TFA 对 V1b 受体的选择性高于对人类 V1a 受体、V2 受体和催产素受体。

d[Cha4]-AVP TFAamp;;

d[Cha4]-AVP TFA Chemical Structure

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d[Cha4]-AVP TFA 的其他形式现货产品:

d[Cha4]-AVP

生物活性

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].

IC50 Target

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

体外研究
(In Vitro)

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.

分子量

1208.33

Formula

C52H72F3N13O13S2

Sequence

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

Sequence Shortening

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

运输条件

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.

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