1-(4-溴苄基)吲哚-2,3-二酮
|
|
|
- CAS号:
- 79183-37-2
- 英文名:
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- 英文别名:
- VU0119498;1-(4-BROMOBENZYL)INDOLE-2,3-DIONE;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
- 中文名:
- 1-(4-溴苄基)吲哚-2,3-二酮
- 中文别名:
- 化合物VU0119498;1-(4-溴苄基)吲哚-2,3-二酮;VU0119498,M 1毒蕈碱受体激动剂
- CBNumber:
- CB82463915
- 分子式:
- C15H10BrNO2
- 分子量:
- 316.15
- MOL File:
- 79183-37-2.mol
|
|
|
1-(4-溴苄基)吲哚-2,3-二酮化学性质
-
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:
-
DMSO: 50 mg/mL (158.15 mM)
-
|
-
形态:
-
A solid
-
|
-
酸度系数(pKa):
-
-2.61±0.20(Predicted)
-
|
1-(4-溴苄基)吲哚-2,3-二酮性质、用途与生产工艺
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.
|
1-(4-溴苄基)吲哚-2,3-二酮
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-114933 | VU0119498 | | 5 mg | 375元 |
| 2024/01/25 | HY-114933 | 1-(4-溴苄基)吲哚-2,3-二酮
VU0119498 | 79183-37-2 | 10mg | 600元 |
79183-37-2, 1-(4-溴苄基)吲哚-2,3-二酮 相关搜索:
- 合成有机化合物配体
- VU0119498,M 1毒蕈碱受体激动剂
- 化合物VU0119498
- 1-(4-溴苄基)吲哚-2,3-二酮
- 79183-37-2
- antidiabetic,VU 0119498,Inhibitor,VU0119498,inhibit,VU-0119498,mAChR,pan,Muscarinic acetylcholine receptor
- 1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]-
- 1-(4-bromobenzyl)-1H-indole-2,3-dione
- VU0119498
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE