Adomeglivant (Synonyms: 阿度格列凡; LY2409021)
目录号: PL04974 纯度: ≥98%
CAS No. :1488363-78-5
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中文名称
Adomeglivant
中文别名
Adomeglivant
英文名称
Adomeglivant
英文别名
Adomeglivant;LY2409021;LY-2409021;Adomeglivant [USAN];74Z5ZL2KVG;Adomeglivant (USAN);3-(4-{(1S)-1-[(4'-tert-butyl-2,6-dimethylbiphenyl-4-yl)oxy]-4,4,4-trifluorobutyl}benzamido)propanoic acid;LY 2409021;GTPL9479;3-[[4-[(1S)-1-[4-(4-tert-butylphenyl)-3,5-dimethylphenoxy]-4,4,4-trifluorobutyl]benzoyl]amino]propanoic acid;DB11704;SB19623;S0555;D10861;Q27266313
Cas No.
1488363-78-5
分子式
C32H36F3NO4
分子量
555.63
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Adomeglivant (LY2409021) 是一种有效的选择性胰高血糖素受体 (GluR) 变构拮抗剂。Adomeglivant 广泛应用于 2 型糖尿病的研究。
生物活性
Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.
性状
Solid
IC50 & Target[1][2]
GluR
体外研究(In Vitro)
Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells.
Adomeglivant fails to block cAMP-elevating actions of adenosine.
Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avp 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.)
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Sonam Grover, et al. Computational identification of novel natural inhibitors of glucagon receptor for checking type II diabetes mellitus. BMC Bioinformatics. 2014; 15(Suppl 16): S13.
[2]. Oleg G Chepurny, et al. 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.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (179.98 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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