1-(4-溴苄基)吲哚-2,3-二酮
| 中文名称 | 1-(4-溴苄基)吲哚-2,3-二酮 |
|---|---|
| 中文同义词 | 1-(4-溴苄基)吲哚-2,3-二酮;化合物VU0119498;VU0119498,M 1毒蕈碱受体激动剂 |
| 英文名称 | 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE |
| 英文同义词 | 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE;VU0119498;1-(4-bromobenzyl)-1H-indole-2,3-dione;1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]-;antidiabetic,VU 0119498,Inhibitor,VU0119498,inhibit,VU-0119498,mAChR,pan,Muscarinic acetylcholine receptor |
| CAS号 | 79183-37-2 |
| 分子式 | C15H10BrNO2 |
| 分子量 | 316.15 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 79183-37-2.mol |
| 结构式 |  |
1-(4-溴苄基)吲哚-2,3-二酮 性质
| 熔点 | 178-180 °C |
|---|---|
| 沸点 | 469.2±47.0 °C(Predicted) |
| 密度 | 1.604±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | 二甲基亚砜：50 mg/mL（158.15 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | -2.61±0.20(Predicted) |
VU0119498 是一种泛Gq muscarinic acetylcholine receptor (mAChR) M1，M3，M5的正向变构调节剂(PAM)，对应EC50值分别为6.1 μM, 6.4 μM, 4.1 μM。
| Target | Value |
|
mAChR M5
(Cell-free assay) | 4.1 μM |
|
mAChR M1
(Cell-free assay) | 6.1 μM |
|
mAChR M3
(Cell-free assay) | 6.4 μM |
VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC
50
s 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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-114933 | VU0119498 | 5 mg | 375元 | |
| 2024/04/30 | HY-114933 | 1-(4-溴苄基)吲哚-2,3-二酮 VU0119498 | 79183-37-2 | 10mg | 600元 |