產(chǎn)品目錄

規(guī)格	10mg 25mg 50mg 100mg
CAS	79183-37-2
別名	N/A
化學(xué)名	N/A
分子式	C15H10BrNO2
分子量	316.15
溶解度	DMSO: 50 mg/mL (158.15 mM)
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)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.

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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