Bay 55-9837

Biological Activity

Bay 55-9837 is a selective VPAC₂ receptor agonist (EC₅₀ values are 0.4, 100 and >1000 nM for VPAC₂, VPAC₁ and PAC₁, respectively in a cAMP accumulation assay; IC₅₀ values are 60, 8700 and >10000 nM for VPAC₂, VPAC₁ and PAC₁, respectively in a competition binding assay). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets. Reduces HIV-1 viral replication and shows cooperative effects when given in conjunction with VPAC₁ agonists.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Macrophage resistance to HIV-1 infection is enhanced by the neuropeptides VIP and PACAP.
   Temerozo et al.
   PLoS ONE, 2013;8:67701
2. A potent and highly selective VPAC2 agonist enhances glucose-induced Ins release and glucose disposal: a potential therapy for type 2 diabetes.
   Tsutsumi et al.
   Diabetes, 2002;51:1453
3. Engineering of a VPAC2 receptor peptide agonist to impart dipeptidyl peptidase IV stability and enhance in vivo glucose disposal.
   Clairmont et al.
   J.Med.Chem., 2006;49:7545
4. Engineering novel VPAC2-selective agonists with improved stability and glucose-lowering activity in vivo.
   Pan et al.
   J.Pharmacol.Exp.Ther., 2007;320:900

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