A 71915

A 71915;

A 71915 是一种具有高效、竞争性的 natriuretic peptide receptor A (ANP, NPRA) 拮抗剂 (pKi= 9.18). A71915 的剂量依赖性取代 [125I]ANP,Ki为0.65 nM。A71915 (pA2= 9.48) 对大鼠 ANP 诱导的 NB-OK-1 细胞产生 cGMP 的作用。

A 71915amp;;

A 71915 Chemical Structure

CAS No. : 132956-87-7

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生物活性

A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells[1].

IC50 Target

A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist, with a pKi of 9.18.

体外研究
(In Vitro)

A 71915 combines to Neuroblastoma NB-OK-1 cells, is used in the Cyclic GMP assay.
A 71915 shifts the ANP dose-response curve of cyclic GMP production to the right[1].

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

体内研究
(In Vivo)

A 71915 (5 μl; i.m.; 25-30 g male CD-1 mice) affects BNP (1 nmol)- and GRP (0.1 nmol)-induced scratching[2].
A 71915 (30 μg/ kg/ day) inhibits NS-398 on blood pressure decreased[3].

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

Animal Model: Rat (Male Sprague-Dawley); weighing 150-180 g[3]
Dosage: 30 μg/kg/day; infused for 3 weeks
Administration: via a mini-osmotic pump
Result: The inhibitory effect of NS-398 on blood pressure was attenuated by the pretreatment with A 71915 (30 μg/kg/day).

分子量

1613.95

Formula

C69H116N26O15S2

CAS 号

132956-87-7

Sequence

Arg-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-D-tic-Arg-Cys-NH2 (Disulfide bridge: Cys2-Cys13)

Sequence Shortening

{RC-Cha}-GGRIDRI-{D-Tic-RC}-NH2 (Disulfide bridge: Cys2-Cys13)

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]. Delporte C, et al. Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line. Eur J Pharmacol. 1992;224(2-3):183-188.

    [2]. Kiguchi N, et al. Spinal Functions of B-Type Natriuretic Peptide, Gastrin-Releasing Peptide, and Their Cognate Receptors for Regulating Itch in Mice.

    [3]. Park BM, et al. Attenuation of renovascular hypertension by cyclooxygenase-2 inhibitor partly through ANP release. Peptides. 2015;69:1-8.