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 |
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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 |
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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) |
颜色 | 橙至红色 |
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 |
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2024/11/08 | HY-114933 | VU0119498 | 5 mg | 375元 | |
2024/11/08 | HY-114933 | 1-(4-溴苄基)吲哚-2,3-二酮 VU0119498 | 79183-37-2 | 10mg | 600元 |