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VU0152100
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。
VU0152100图片
CAS NO:409351-28-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
VU152100
产品介绍
VU0152100 是一种选择性 M4 mAChR 变构增强剂,EC50为 380 ± 93 nM。

产品描述

VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).

体外活性

VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1].

体内活性

Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1].

Cas No.

409351-28-6

分子式

C18H19N3O2S

分子量

341.43

别名

VU152100;VU0152100

储存和溶解度

DMSO:45 mg/mL (131.80 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years