• 产品描述： VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity

• 靶点： mAChR;AChR

• 体外研究：
  VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells. VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets

• 体内研究：
  VU0119498 (0.1-2 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in mice in a β-cell M3R-dependent fashion. VU0119498 (0.5 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in obese, glucose-intolerant mice. Animal Model: Male WT mice (12 weeks) Dosage: 0.1, 0.5, 2 mg/kg Administration: A single i.p. Result: Caused a significant improvement in glucose tolerance at the dose of 0.5 mg/kg.Significantly augmented GSIS at the dose of 0.5 mg/kg.

• 参考文献：
  1. Bridges TM, et, al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. 2. Bridges TM, et, al. Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1972-5. 3. Zhu L, et, al. Allosteric modulation of β-cell M 3 muscarinic acetylcholine receptors greatly improves glucose homeostasis in lean and obese mice. Proc Natl Acad Sci U S A. 2019 Sep 10;116(37):18684-18690.

• 溶解性： Soluble  in  DMSO

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.163 ml	15.815 ml	31.63 ml
  5 mM	0.633 ml	3.163 ml	6.326 ml
  10 mM	0.316 ml	1.582 ml	3.163 ml
  50 mM	0.063 ml	0.316 ml	0.633 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 *