79183-37-2
中文名稱
1-(4-溴芐基)吲哚-2,3-二酮
英文名稱
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
CAS
79183-37-2
分子式
C15H10BrNO2
分子量
316.15
MOL 文件
79183-37-2.mol
更新日期
2024/12/15 19:35:20
79183-37-2 結(jié)構(gòu)式
基本信息
中文別名
化合物VU01194981-(4-溴芐基)吲哚-2,3-二酮
英文別名
VU01194981-(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
物理化學(xué)性質(zhì)
熔點(diǎn)178-180 °C
沸點(diǎn)469.2±47.0 °C(Predicted)
密度1.604±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Room Temperature
溶解度DMSO: 50 mg/mL (158.15 mM)
酸度系數(shù)(pKa)-2.61±0.20(Predicted)
形態(tài)固體
顏色Orange to red
常見(jiàn)問(wèn)題列表
生物活性
VU0119498 是一種泛Gq muscarinic acetylcholine receptor (mAChR) M1，M3，M5的正向變構(gòu)調(diào)節(jié)劑(PAM)，對(duì)應(yīng)EC50值分別為6.1 μM, 6.4 μM, 4.1 μM。靶點(diǎn)
| 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 |
體外研究
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.
體內(nèi)研究
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. |