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.
体外研究
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.
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.
体内研究
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.
分子式
C15H10NO2Br
分子量
316.15
CAS号
79183-37-2
运输条件
Room temperature in continental US; may vary elsewhere.