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
[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