VU0119498
目录号: PL06878 纯度: ≥99%
CAS No. :79183-37-2
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PL06878-10mg 10mg ¥741.82 请登录
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中文名称
VU0119498
英文名称
VU0119498
英文别名
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE;1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]-;VU0119498
Cas No.
79183-37-2
分子式
C15H10NO2Br
分子量
316.15
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
VU0119498 是一种泛 Gq mAChR M1,M3,M5 的正变构调节剂 (PAM),EC50 值分别为 6.04,6.38 和 4.08 µM。VU0119498 具有抗糖尿病活性。
生物活性
VU0119498 is a pan G q mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC 50 s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity.
性状
Solid
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (158.15 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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