AC 187

AC 187 是一种有效且具有口服活性的胰淀素受体拮抗剂，IC50 为 0.48 nM，Ki 为 0.275 nM。

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Background

Amylin is a 37-amino acid peptide co-secreted with insulin from pancreatic β-ells. The plasma concentration of amyline increases with nutrient stimuli. AC187 is a potent amylin antagonist

In vitro: AC187 potently competes for rat amylin binding at high affinity sites such as rat nucleus accumbens membranes which have been useful in developing a number of selective ligands, including AC187. The Kd for amylin at this site is 28 pM, and the Ki for AC187 is 79 pM. AC187 is relatively selective in competing for amylin binding, displacing amylin from nucleus accumbens membranes with over 400-fold greater potency [1].

In vivo: AC187 was able to inhibit metabolic responses to exogenous amylin in the intact animal. An infusion of AC187 that was itself without effect on lactate levels in anesthetized rats, inhibited by more than 90% the lactate increment evoked by infusions of rat amylin. Other experiments have shown that AC187-induced amylin blockade action is surmountable by higher doses of amylin, indicative of a competitive antagonism [1].

Clinical trial: Up to now, AC187 is still in the preclinical development stage.

Reference:
[1] Young AA, Gedulin B, Gaeta LS, Prickett KS, Beaumont K, Larson E, Rink TJ.? Selective amylin antagonist suppresses rise in plasma lactate after intravenous glucose in the rat. Evidence for a metabolic role of endogenous amylin. FEBS Lett. 1994 May 2;343(3):237-41.