AC 187 TFA
目录号: PL05844 纯度: ≥99%
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中文名称
AC 187 TFA
英文名称
AC 187 TFA
包装储存
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
产品详情
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。
生物活性
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC 50 of 0.48 nM and a K i of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects.
性状
Solid
IC50 & Target[1][2]
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.
AC187 attenuates the activation of initiator and effector caspases that mediate Aβ-induced apoptotic cell death. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
SequenceShortening
Ac-VLGKLSQELHKLQTYPRTNTGSNTY-NH2
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
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.
溶解度数据
In Vitro: H2O : 100 mg/mL (33.29 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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