VU0119498 | mAChR M1/3/5 PAM | AmBeed-信号通路专用抑制剂

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VU0119498 {[allProObj[0].p_purity_real_show]}

货号：A929093

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.

VU0119498 化学结构
CAS号：79183-37-2

VU0119498 3D分子结构
CAS号：79183-37-2

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VU0119498 纯度/质量文件产品仅供科研

货号：A929093 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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AChR 亚型比较

产品名称	AChE ↓ ↑	AChR ↓ ↑	mAChR ↓ ↑	nAChR ↓ ↑	其他靶点	纯度
Donepezil	+++ bAChE, IC50: 8.12 nM hAChE, IC50: 11.6 nM					98%
Loganin	++ AChE, IC50: 3.95 μM					99%+
topride HCl	++ AChE, IC50: 2.04 μM					98%
Dehydroevodiamine HCl	✔					99%+
Jatrorrhizine	++ AChE, IC50: 872 nM					99%+
Palmatine	++ AChE, IC50: 0.51 μM					95%
(-)-Huperzine A	++++ AChE (G4 form), Ki: 7 nM					98%
Galanthamine HBr	++ AChE, IC50: 0.35 μM					98%
Trospium chloride		✔				99%
Tiotropium Bromide Monohydrate		✔				97%
Gallamine Triethiodide		+ AChR, IC50: 68.0 μM				98%
Hexamethonium Bromide		✔				99%
Pancuronium dibromide		✔				98%
Neostigmine bromide		✔				98%
Orphenadrine citrate		✔				98%
Oxybutynin		✔				98%
Irsogladine		✔			PDE	99%
Pyridostigmine bromide		✔				99+%
Rivastigmine		+ AChR, IC50: 5.5 μM				98%
Paroxetine HCl		✔				99%
Rocuronium Bromide		✔				98%
Tropicamide			+++ M4 mAChR, IC50: 8 nM			98%
Diphenmanil methylsulfate			✔			99%
Umeclidinium bromide			✔			95%
Otilonium bromide			✔			98%
Flavoxate HCl			+ mAChR, IC50: 12.2 μM			99%
Ipratropium bromide			✔			98%
Diphenidol HCl			✔			98%
Darifenacin hydrobromide			++++ M3 mAChR, pKi: 8.9			98%
Aclidinium Bromide			++++ M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 nM			98%
Oxybutynin chloride			✔			99%
Pentoxyverine citrate			✔			98%
Solifenacin			✔			98%
Catharanthine				✔		98%
Benzethonium chloride				+++ α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM		99+%
Vinblastine sulfate				+ nAChR, IC50: 8.9 μM		99%
PNU-120596				++ α7 nAChR, EC50: 216 nM		99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

VU0119498 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].

VU0119498 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

VU0119498 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.82mL

3.16mL

1.58mL

31.63mL

6.33mL

3.16mL

VU0119498 技术信息

CAS号	79183-37-2
分子式	C₁₅H₁₀BrNO₂
分子量	316.15
SMILES Code	O=C1N(CC2=CC=C(Br)C=C2)C3=C(C=CC=C3)C1=O
MDL No.	MFCD01538528

别名
运输	蓝冰
InChI Key	DELLOEULSHGYCG-UHFFFAOYSA-N
Pubchem ID	3008304

存储条件	In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, room temperature

VU0119498 {[allProObj[0].p_purity_real_show]}

VU0119498 纯度/质量文件产品仅供科研

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VU0119498 {[allProObj[0].p_purity_real_show]}

VU0119498 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

VU0119498 质控信息

VU0119498 生物活性

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VU0119498 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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VU0119498 纯度/质量文件产品仅供科研