AC 187

Potent and selective amylin receptor antagonist that displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Through attenuating the activation of initiator and effector caspases in vitro, it blocks amyloid β-induced neurotoxicity. It can increase glucagon secretion, accelerate gastric emptying, change plasma glucose levels and increase food intake in vivo.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
AC 187(CAS 151804-77-2)

CAT No: R0952

CAS No:151804-77-2

Synonyms/Alias:151804-77-2;AC 187;AC187;salmon calcitonin (8-32) reduced;CID 16133792;GTPL689;AKOS024457619;acetyl-(Asn30,Tyr32)-calcitonin8-32;FA109403;Acetyl-(Asn30,Tyr32)-Calcitonin (8-32) (salmon I) trifluoroacetate salt;161902-50-7;

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cGMP Peptide
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M.F/Formula
C127H205N37O40
M.W/Mr.
2890.2
Sequence
One Letter Code:VLGKLSQELHKLQTYPRTNTGSNTY
Three Letter Code:Ac-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Asn-Thr-Tyr-NH2
Labeling Target
Amylin receptor
Application
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.
Appearance
White lyophilised solid
Purity
>98%
Activity
Antagonist

AC 187 is a synthetic peptide compound recognized for its role as a selective antagonist of amylin receptors. As a linear peptide, it is structurally designed to interact with the amylin receptor complex, thereby modulating the physiological effects mediated by the endogenous peptide hormone amylin. Its specificity and well-characterized mechanism of action make AC 187 a valuable tool in the investigation of amylin signaling pathways, metabolic regulation, and peptide-receptor interactions. The compound is widely utilized in biochemical research settings to elucidate the functional roles of amylin and related peptides in both cellular and organismal models.

Receptor binding studies: AC 187 serves as a reference antagonist in receptor binding assays aimed at characterizing amylin receptor pharmacology. By selectively inhibiting amylin-induced signaling, it enables researchers to delineate the binding affinities and specificities of novel ligands or receptor subtypes. Its use in competitive binding experiments helps clarify receptor-ligand dynamics and supports the development of new amylin-targeted compounds for basic research applications.

Signal transduction analysis: The compound is instrumental in dissecting intracellular signaling cascades initiated by amylin receptor activation. By blocking amylin-mediated responses, AC 187 allows investigators to map downstream effectors and second messenger systems, such as cyclic AMP pathways or calcium fluxes. This application is critical for understanding the molecular basis of amylin's physiological actions and for identifying potential regulatory nodes within metabolic signaling networks.

Metabolic pathway research: AC 187 is frequently utilized in studies examining the regulation of glucose metabolism, energy homeostasis, and related endocrine functions. By antagonizing amylin activity, it helps clarify the distinct contributions of amylin signaling in metabolic processes, including insulin secretion, appetite regulation, and nutrient partitioning. Its use in both in vitro and ex vivo models facilitates the dissection of complex metabolic pathways influenced by peptide hormones.

Peptide-receptor interaction studies: As a structurally defined amylin receptor antagonist, AC 187 provides a reliable probe for investigating the structural determinants of peptide-receptor recognition. Researchers employ it to explore the conformational requirements for receptor binding and to assess the role of specific amino acid residues in ligand selectivity. These studies contribute to a deeper understanding of peptide structure-activity relationships and inform the rational design of next-generation peptide modulators.

Pharmacological profiling: The compound is also employed in the functional characterization of amylin receptor subtypes across different tissue types and species. By serving as a pharmacological tool, AC 187 aids in distinguishing receptor isoforms and evaluating their physiological relevance. This application is essential for expanding knowledge of peptide hormone signaling diversity and for guiding future research efforts in peptide-based modulation of metabolic and neuroendocrine systems.

Source#
Synthetic
Long-term Storage Conditions
Soluble in water
InChI
InChI=1S/C127H205N37O40/c1-59(2)44-81(156-122(200)99(63(9)10)142-68(15)171)105(183)139-54-96(178)143-74(22-16-18-40-128)106(184)151-84(47-62(7)8)114(192)159-90(57-166)119(197)148-77(34-37-92(130)174)108(186)146-79(36-39-98(180)181)109(187)153-83(46-61(5)6)113(191)154-85(50-71-53-137-58-141-71)115(193)145-75(23-17-19-41-129)107(185)152-82(45-60(3)4)112(190)147-78(35-38-93(131)175)111(189)162-103(67(14)170)125(203)158-88(49-70-28-32-73(173)33-29-70)126(204)164-43-21-25-91(164)120(198)149-76(24-20-42-138-127(135)136)110(188)161-102(66(13)169)124(202)157-87(52-95(133)177)117(195)160-100(64(11)167)121(199)140-55-97(179)144-89(56-165)118(196)155-86(51-94(132)176)116(194)163-101(65(12)168)123(201)150-80(104(134)182)48-69-26-30-72(172)31-27-69/h26-33,53,58-67,74-91,99-103,165-170,172-173H,16-25,34-52,54-57,128-129H2,1-15H3,(H2,130,174)(H2,131,175)(H2,132,176)(H2,133,177)(H2,134,182)(H,137,141)(H,139,183)(H,140,199)(H,142,171)(H,143,178)(H,144,179)(H,145,193)(H,146,186)(H,147,190)(H,148,197)(H,149,198)(H,150,201)(H,151,184)(H,152,185)(H,153,187)(H,154,191)(H,155,196)(H,156,200)(H,157,202)(H,158,203)(H,159,192)(H,160,195)(H,161,188)(H,162,189)(H,163,194)(H,180,181)(H4,135,136,138)/t64-,65-,66-,67-,74+,75+,76+,77+,78+,79+,80+,81+,82+,83+,84+,85+,86+,87+,88+,89+,90+,91+,99+,100+,101+,102+,103+/m1/s1
InChI Key
ZLFXHYNEZYAYPG-AABHONRUSA-N
Isomeric SMILES
C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC=N4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)C)O
BoilingPoint
N/A
Melting Point
N/A

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