VU0119498

Research use only, not for human use.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3 M5 positive allosteric modulator (PAM)and is a neuroprotective agent.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3 M5 positive allosteric modulator (PAM)and is a neuroprotective agent.

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.

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.

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Endocrinology/Hormones

AChR

mAChR

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79183-37-2

316.15

C15H10BrNO2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (158.15 mM)

Brc1ccc(CN2C(=O)C(=O)c3ccccc23)cc1

1-[(4-bromophenyl)methyl]indole-23-dione

(-20℃)

With Ice Pack

≥ 2 years