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AC 187

Cat. No. 3419

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Biological Activity

Orally active, potent amylin receptor antagonist (IC₅₀ = 0.48 nM) that displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Blocks amyloid β-induced neurotoxicity by attenuating the activation of initiator and effector caspases in vitro. Increases glucagon secretion, accelerates gastric emptying, alters plasma glucose levels and increases food intake in vivo.

Technical Data

M.Wt:

2890.25

Formula:

C₁₂₇H₂₀₅N₃₇O₄₀

Sequence:

VLGKLSQELHKLQTYPRTNTGSNTY

(Modifications: Val-1 = N-terminal Ac, Tyr-25 = C-terminal amide)

Solubility:

Soluble to 1 mg/ml in 20% acetonitrile - 0.1% acetic acid

Storage:

Desiccate at -20°C

CAS No:

151804-77-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Jhamandas and MacTavish (2004) Antagonist of the amylin receptor blocks β-amyloid toxicity in rat cholinergic basal forebrain neurons. J.Neurosci. 24 5579. PMID: 15201330.

Reidelberger et al (2004) Amylin receptor blockade stimulates food intake in rats. Am.J.Physiol.Inter.Comp.Physiol. 287 R568.

Gedulin et al (2006) Role of endogenous amylin in glucagon secretion and gastric emptying in rats demonstrated with the selective antagonist, AC187. Regul.Pept. 137 121. PMID: 16914214.

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