| Bioactivity | AC 253, an amylin antagonist, inhibits 125I-adrenomedullin binding, with an IC50 of 25 nM[1]. |
| Invitro | AC 253 (5-20 μM) antagonizes adrenomedullin-stimulated cAMP production at micromolar concentrations[1].AC 253 (5-10 μM) blocks increases in intracellular Ca2+, activation of protein kinase A, MAPK, Akt, cFos, and cell death, which occur upon AMY3 activation with hAmylin, Aβ1-42, or their co-application[2].AC 253 (10 nM) blocks Aβ1-42-induced electrophysiological effects[3]. |
| Name | AC 253 |
| CAS | 151804-79-4 |
| Sequence | Ac-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Asn-Thr-Tyr-NH2 |
| Shortening | Ac-LGRLSQELHRLQTYPRTNTGSNTY-NH2 |
| Formula | C122H196N40O39 |
| Molar Mass | 2847.11 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. H A Coppock, et al. Rat-2 fibroblasts express specific adrenomedullin receptors, but not calcitonin-gene-related-peptide receptors, which mediate increased intracellular cAMP and inhibit mitogen-activated protein kinase activity. Biochem J. 1999 Feb 15;33 [2]. Wen Fu, ET AL. Amyloid β (Aβ) peptide directly activates amylin-3 receptor subtype by triggering multiple intracellular signaling pathways. J Biol Chem. 2012 May 25;287(22):18820-30. [3]. Jack H Jhamandas, et al. Actions of β-amyloid protein on human neurons are expressed through the amylin receptor. Am J Pathol. 2011 Jan;178(1):140-9. |