货号	规格	价格	上海	北京	珠海	重庆	武汉
S89246-5mg买3赠1	99.40%	￥160.00 S89246-5mg ￥160.00 现货（买3赠1）	5 5	-	-	-	-
S89246-10mg买3赠1	99.40%	￥270.00 S89246-10mg ￥270.00 现货（买3赠1）	5 5	-	-	-	-
S89246-25mg买3赠1	99.40%	￥500.00 S89246-25mg ￥500.00 现货（买3赠1）	5 5	-	-	-	-
S89246-100mg促销	99.40%	￥1070.00 ￥856.00 S89246-100mg ￥856.00 现货	3 3	-	-	-	-

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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：

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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