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首页-小分子抑制剂&激动剂-GPCR-Vasoactive intestinal peptide receptor (VIPR)-VPAC2 antagonist 1
VPAC2 antagonist 1

Chemical Structure : VPAC2 antagonist 1

CAS No.: 1213241-72-5

VPAC2 antagonist 1

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 539.60
分子式 C27H29N3O7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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