AC 187 TFA

AC 187 TFA; 纯度: 99.56%

AC 187 TFA 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 TFA 对胰淀素受体的选择性高于降钙素和 CGRP 受体。AC 187 TFA 具有神经保护作用。

AC 187 TFAamp;;

AC 187 TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
25 mg ¥9700 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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生物活性

AC 187 TFA 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 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA 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

3004.27

Formula

C129H206F3N37O42

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

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 100 mg/mL (33.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3329 mL 1.6643 mL 3.3286 mL
5 mM 0.0666 mL 0.3329 mL 0.6657 mL
10 mM 0.0333 mL 0.1664 mL 0.3329 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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.

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