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
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M.Wt
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539.60
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Formula
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C27H29N3O7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Alan Chu, et al. Mol Pharmacol. 2010 Jan;77(1):95-101.
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