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VU0119498
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
VU0119498图片
CAS NO:79183-37-2
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
VU0119498是一种泛GqmAChRM1，M3，M5的正变构调节剂(PAM)，EC50值分别为6.04，6.38和4.08µM。VU0119498具有抗糖尿病活性。
Cas No.79183-37-2
别名1-(4-溴苄基)吲哚-2,3-二酮
Canonical SMILESO=C1N(C2=C(C1=O)C=CC=C2)CC3=CC=C(C=C3)Br
分子式C15H10BrNO2
分子量316.15
溶解度DMSO: 50 mg/mL (158.15 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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[1][2][3].

VU0119498 (0.01-30 μM; 150s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC50s of 6.04, 6.38, and 4.08 µM, respectively[1].VU0119498 (3-20 μM) augments ACh-mediated increases in insulin secretion and intracellular calcium levels in MIN6-K8 cells[3].VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets[3].

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[3].VU0119498 (0.5 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in obese, glucose-intolerant mice[3]. Animal Model: Male WT mice (12 weeks)[3]

[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.