|1-(4-溴苄基)吲哚-2,3-二酮|CsnPharm

CAS No.: 79183-37-2

VU0119498 Catalog No. CSN27586

VU0119498 is a M1 muscarinic receptor agonist with EC50 of 3.1 μM, and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

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实验方案

技术信息

生物活性

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^[2]. 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. VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets. VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells^[3].
参考文献

[1] Bridges TM, Marlo JE, Niswender CM, 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;52(11):3445-3448.
[2] Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. 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
[3] Zhu L, Rossi M, Cohen A, Pham J, Zheng H, Dattaroy D, Mukaibo T, Melvin JE, Langel JL, Hattar S, Matschinsky FM, Appella DH, Doliba NM, Wess J. Allosteric modulation of β-cell M3 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1631 mL
- 15.8153 mL
- 31.6306 mL
- 5 mM
- 0.6326 mL
- 3.1631 mL
- 6.3261 mL
- 10 mM
- 0.3163 mL
- 1.5815 mL
- 3.1631 mL

技术信息

CAS号

79183-37-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H10BrNO2

运输

蓝冰

分子量

316.15

别名

溶解度

DMSO	50.0 mg/mL (158.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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