AC 187

AC 187;

AC 187 是一种有效且具有口服活性的胰淀素受体 (amylin receptor) 拮抗剂,IC50 为 0.48 nM,Ki 为 0.275 nM。AC 187 对胰淀素受体的选择性高于降钙素和 CGRP 受体。AC 187 具有神经保护作用。

AC 187amp;;

AC 187 Chemical Structure

CAS No. : 151804-77-2

规格 是否有货
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AC 187 的其他形式现货产品:

AC 187 TFA

生物活性

AC 187 is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects[1][2].

IC50 Target

IC50: 0.48 nM (amylin receptor)

体外研究
(In Vitro)

AC 187 blocks amyloidβ protein (Aβ)-induced neurotoxicity. Treatment of cultures with AC 187 before exposure to Aβ results in significantly improved neuronal survival[1].
AC187 attenuates the activation of initiator and effector caspases that mediate Aβ-induced apoptotic cell death[1].

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

体内研究
(In Vivo)

AC 187 (30 mg/mL) increases glucagon concentration, accelerates gastric emptying of liquids, and results in an exaggerated post-challenge glycemia in hyperinsulinemic clamps in Sprague-Dawley (HSD) rats[2].

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

分子量

2890.25

Formula

C127H205N37O40

CAS 号

151804-77-2

Sequence

Ac-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Asn-Thr-Tyr-NH2

Sequence Shortening

Ac-VLGKLSQELHKLQTYPRTNTGSNTY-NH2

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]. Jack H Jhamandas, et al. Antagonist of the amylin receptor blocks beta-amyloid toxicity in rat cholinergic basal forebrain neurons. J Neurosci. 2004 Jun 16;24(24):5579-84.

    [2]. Bronislava R Gedulin, et al. Role of endogenous amylin in glucagon secretion and gastric emptying in rats demonstrated with the selective antagonist, AC187. Regul Pept. 2006 Dec 10;137(3):121-7.