Name | 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE |
---|---|
Synonyms | VU0119498 |
Description | VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity[1][2][3]. |
---|---|
Related Catalog | |
In Vitro | VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC50s of 6.04, 6.38, and 4.08 µM, respectively[1]. VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells[3]. VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets[3]. |
In Vivo | 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[3]. VU0119498 (0.5 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in obese, glucose-intolerant mice[3]. Animal Model: Male WT mice (12 weeks)[3] 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. |
References |
Molecular Formula | C15H10BrNO2 |
---|---|
Molecular Weight | 316.153 |
Storage condition | -20°C |
Hazard Codes | Xn |
---|