| CAS NO: | 1488363-78-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Name: Adomeglivant CAS#: 1488363-78-5 Chemical Formula: C32H36F3NO4 Exact Mass: 555.2596 Molecular Weight: 555.64 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: LY-2409021; LY2409021; LY 2409021 Chemical Name: 3-(4-{(1S)-1-[(4'-tert-butyl-2,6-dimethylbiphenyl-4-yl)oxy]-4,4,4-trifluorobutyl}benzamido)propanoic acid InChi Key: FASLTMSUPQDLIB-MHZLTWQESA-N InChi Code: InChI=1S/C32H36F3NO4/c1-20-18-26(19-21(2)29(20)23-10-12-25(13-11-23)31(3,4)5)40-27(14-16-32(33,34)35)22-6-8-24(9-7-22)30(39)36-17-15-28(37)38/h6-13,18-19,27H,14-17H2,1-5H3,(H,36,39)(H,37,38)/t27-/m0/s1 SMILES Code: O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C3=CC=C(C(C)(C)C)C=C3)C(C)=C2)CCC(F)(F)F)C=C1)=O |
In Vitro : Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells[2]. Adomeglivant fails to block cAMP-elevating actions of adenosine[2].
Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R.
In Vivo: Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avpires-Cre+ mice. (CNO is a specific, pharmacologically inert agonist for hM3Dq-induced membrane depolarisation and increased the firing rate in hM3Dq-expressing arginine-vasopressin (AVP) neurons.)[3]
References:
[1]. Computational identification of novel natural inhibitors of glucagon receptor for checking type II diabetes mellitus. BMC Bioinformatics. 2014; 15(Suppl 16): S13.
[2]. Non-conventional glucagon and GLP-1 receptor agonist and antagonist interplay at the GLP-1 receptor revealed in high-throughput FRET assays for cAMP. J Biol Chem. 2019 Mar 8;294(10):3514-3531.
[3]. AVP-induced counter-regulatory glucagon is diminished in type 1 diabetes. bioRxiv. January 31, 2020.
[4]. Efficient Synthesis of β-CF3/SCF3-Substituted Carbonyls via Copper-Catalyzed Electrophilic Ring-Opening Cross-Coupling of Cyclopropanols. Org Lett. 2015 May 1;17(9):2186-9.
[5]. Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies. Diabetes Care. 2016 Jul;39(7):1241-9
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