AC 187

- Overview
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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.
- Properties
  - Categories
    
    Amylin receptor antagonist, Potent and selective
    
    CAS Number
    
    151804-77-2
    
    Molecular Formula
    
    C127H205N37O40
    
    Molecular Weight
    
    2890.25
    
    Appearance
    
    White lyophilised solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble to 1 mg/ml in H2O
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

AC 187

Background

Documents

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