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VPAC2 antagonist 1

Chemical Structure : VPAC2 antagonist 1

CAS No.: 1213241-72-5

VPAC2 antagonist 1

Catalog No.: PC-20663Not For Human Use, Lab Use Only.

VPAC2 antagonist 1 is a small molecule human vsoactive intestinal peptide receptor-2 (hVIPR2, hVPAC2 receptor) antagonist, inhibits VPAC2-mediated cAMP accumulation with IC50 of 3.8 uM and the ligand-activated beta-arrestin2 binding with IC50 of 2.3 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

VPAC2 antagonist 1 is a small molecule human vsoactive intestinal peptide receptor-2 (hVIPR2, hVPAC2 receptor) antagonist, inhibits VPAC2-mediated cAMP accumulation with IC50 of 3.8 uM and the ligand-activated beta-arrestin2 binding with IC50 of 2.3 uM.
VPAC2 antagonist 1 is a specific VPAC2 antagonist with no detectable agonist or antagonist activities on VPAC(1) or PAC(1).
VPAC2 antagonist 1 is completely inactive on the closely related mouse VPAC2.
VPAC2 antagonist 1 is the first small molecular antagonist that is specific for VPAC(2), and the only VPAC(2) antagonist molecule known to date that allosterically interacts with the 7TM region.

Physicochemical Properties

M.Wt 539.60
Formula C27H29N3O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(N[C@@H]1[C@H](O)CC2=C1C=CC=C2)[C@H](CC3=CC=CC=C3)C[C@H](O)CNS(=O)(C4=CC=C([N+]([O-])=O)C=C4)=O

References

1. Alan Chu, et al. Mol Pharmacol. 2010 Jan;77(1):95-101.

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