Biological Activity
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
| M. Wt | 3742.29 |
| Formula | C167H270N52O46 |
| Sequence |
HSDAVFTDNYTRLRKQVAAKKYLQSIKNKRY (Modifications: Tyr-31 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 463930-25-8 |
| PubChem ID | 72941824 |
| InChI Key | NHMJBXFCQMBYCP-ZBLLYJRDSA-N |
| Smiles | [H]N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3742.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.27 mL | 1.34 mL | 2.67 mL |
| 5 mM | 0.05 mL | 0.27 mL | 0.53 mL |
| 10 mM | 0.03 mL | 0.13 mL | 0.27 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.05 mL |
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References
References are publications that support the products' biological activity.
Tsutsumi et al (2002) A potent and highly selective VPAC2 agonist enhances glucose-induced insulin release and glucose disposal: a potential therapy for type 2 diabetes. Diabetes 51 1453 PMID: 11978642
Clairmont et al (2006) Engineering of a VPAC2 receptor peptide agonist to impart dipeptidyl peptidase IV stability and enhance in vivo glucose disposal. J.Med.Chem. 49 7545 PMID: 17149884
Pan et al (2007) Engineering novel VPAC2-selective agonists with improved stability and glucose-lowering activity in vivo. J.Pharmacol.Exp.Ther. 320 900 PMID: 17110523
Temerozo et al (2013) Macrophage resistance to HIV-1 infection is enhanced by the neuropeptides VIP and PACAP. PLoS ONE 8 67701 PMID: 23818986
Keywords: BAY 55-9837, supplier, Potent, selective, VPAC2, agonists, Vasoactive, Intestinal, Peptide, Receptors, VPAC, VIP, BAY55-9837, VIP, Receptors, Antivirals, VIP, Receptors, Tocris Bioscience
