VU0357017
| 中文名称 | VU0357017 |
|---|---|
| 中文同义词 | 盐酸 VU 0357017;VU 0357017盐酸盐;4-((2-(2-甲基苯甲酰氨基)乙基)氨基)哌啶-1-羧酸乙酯盐酸盐;优选]VU 0357017 HYDROCHLORIDE |
| 英文名称 | VU 0357017 hydrochloride |
| 英文同义词 | VU 0357017 hydrochloride;4-[[2-[(2-Methylbenzoyl)aMino]ethyl]aMino]-1-piperidinecarboxylic Acid Ethyl Ester Hydrochloride;4-[[2-[(2-Methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid ethyl ester monohydrochloride;CID 25010775;Ethyl 4-(2-(2-methylbenzamido)ethylamino)piperidine-1-carboxylate hydrochloride;ML071 hydrochloride;SID 56353039;VU0357017 monohydrochloride |
| CAS号 | 1135242-13-5 |
| 分子式 | C18H28ClN3O3 |
| 分子量 | 369.9 |
| EINECS号 | |
| 相关类别 | 抑制剂;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Positive allosteric modulator of muscarinic M1 receptors.;Amines |
| Mol文件 | 1135242-13-5.mol |
| 结构式 |  |
VU0357017 性质
| 储存条件 | Inert atmosphere,2-8°C |
|---|---|
| 溶解度 | 二甲基亚砜：≥10mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至类白色 |
VU0357017 hydrochloride (CID-25010775)是一种强效的、中枢神经系统渗透性的高选择性 M1 激动剂，M1是 muscarinic acetylcholine receptors (mAChRs) 的一类亚型。VU0357017 hydrochloride 可在变构位点起作用以激活该受体，其EC50值为 477 nM 和 Ki值为 9.91 μM。
| Target | Value |
|
M1 mAChR
(Cell-free assay) | 477 nM(EC50) |
|
M1 mAChR
(Cell-free assay) | 9.91 μM(Ki) |
VU0357017 is selective for M
1
(K
i
=9.91 µM) over M
2
-M
5
mAChRs (K
i
=21.4, 55.3, 35.0, and 50.0 μM, respectively) in CHO cells.
VU0357017 (1 nM-100 μM) induces calcium release and ERK phosphorylation in a concentration-dependent manner in CHO cells.
VU0357017 (1-10 mg/kg, i.p.) reverses scopolamine-induced disruption of the contextual fear conditioning response.
| Animal Model: | Male Sprague−Dawley rats (380-420 g) were pretreated with scopolamine |
| Dosage: | 1, 3, 10 mg/kg |
| Administration: | A single i.p. |
| Result: | Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19752A | VU0357017 VU0357017 hydrochloride | 1135242-13-5 | 5mg | 700元 |
| 2024/01/25 | HY-19752A | VU0357017 VU0357017 hydrochloride | 1135242-13-5 | 10mM * 1mLin DMSO | 770元 |