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• 產(chǎn)品描述： Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus

• 靶點(diǎn)： GluR;GlucagonReceptor

• 體外研究：
  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

• 體內(nèi)研究：
  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.) Animal Model: Avpires-Cre+ mice Dosage: 5 mg/kg Administration: Intraperitoneal injection, 30 minutes prior to CNO Result: Completely abolished the hyperglycaemic action of CNO.

• 參考文獻(xiàn)：
  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. 3. Angela Kim, et al. AVP-induced counter-regulatory glucagon is diminished in type 1 diabetes. bioRxiv. January 31, 2020.

• 溶解性： soluble  in  DMSO

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	1.8 ml	8.999 ml	17.998 ml
  5 mM	0.36 ml	1.8 ml	3.6 ml
  10 mM	0.18 ml	0.9 ml	1.8 ml
  50 mM	0.036 ml	0.18 ml	0.36 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *