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) |
| Storage | Desiccate at -20°C |
| CAS Number | 151804-77-2 |
| PubChem ID | 16133792 |
| InChI Key | ZLFXHYNEZYAYPG-AABHONRUSA-N |
| Smiles | CC(C)C[C@H](NC(=O)[C@@H](NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 2890.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.35 mL | 1.73 mL | 3.46 mL |
| 5 mM | 0.07 mL | 0.35 mL | 0.69 mL |
| 10 mM | 0.03 mL | 0.17 mL | 0.35 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.07 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
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
Reidelberger et al (2004) Amylin receptor blockade stimulates food intake in rats. Am.J.Physiol.Inter.Comp.Physiol. 287 R568 PMID:
Keywords: AC 187, supplier, Potent, selective, amylin, receptors, antagonists, AC187, Calcitonin, and, Related, Receptors, Calcitonin, and, Related, Receptors, Tocris Bioscience
