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

• 靶点： GluR;GlucagonReceptor

• 体外研究：
  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

• 体内研究：
  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.

• 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. 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

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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