• 产品描述： Danuglipron (PF-06882961) 是一种非肽激动剂，仅在具有Trp33ECD的 Glucagon-like peptide-1 (GLP-1) receptor 中激活 canonical G protein 信号传导活性

• 靶点： GLP-1 receptor;GlucagonReceptor

• 体外研究：
  PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R

• 体内研究：
  PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys

• 细胞实验： Cell lines: HEK293 cells Concentrations: 1 μM Incubation Time: 30 minutes Method: HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA

• 动物实验： Animal Models: male cynomolgus monkeys Dosages: 1 mg/kg, 5 mg/kg, 100 mg/kg Administration: IV, Oral gavage

• 参考文献：
  1. Hun Jee Choe, Young Min Cho. Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists. Endocrinol Metab (Seoul). 2021 Feb;36(1):22-29. 2. Griffith DA, et al. A small-molecule oral agonist of the human glucagon-like peptide-1 receptor. bioRxiv. 2020 Sep 30.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.8 ml	8.999 ml	17.999 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 *