| AC 187Amylin receptor antagonist, Potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 151804-77-2 | SDF | Download SDF |
| Canonical SMILES | N/A | ||
| Formula | C127H205N37O40 | M.Wt | 2890.25 |
| Solubility | Soluble to 1 mg/ml in H2O | Storage | Desiccate at -20°C |
| Physical Appearance | White lyophilised solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
