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Merck
CN

182707

GNF351

≥98% (HPLC), solid, AhR antagonist, Calbiochem®

别名:

AhR Antagonist III, GNF351, N-(2-(3H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methyl-3-pyridyl)-7H-purin-6-amine, N-(2-(1H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine

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关于此项目

经验公式（希尔记法）:
C24H25N7
化学文摘社编号:
1227634-69-6
分子量:
411.50
MDL number:
MFCD23726597
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

AhR Antagonist III, GNF351, AhR Antagonist III, GNF351, is a cell-permeable, high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR).

SMILES string

[n]1(c2nc(nc(c2nc1)NCCc4c5c([nH]c4)cccc5)c3cncc(c3)C)C(C)C

InChI

1S/C24H25N7/c1-15(2)31-14-28-21-23(26-9-8-17-13-27-20-7-5-4-6-19(17)20)29-22(30-24(21)31)18-10-16(3)11-25-12-18/h4-7,10-15,27H,8-9H2,1-3H3,(H,26,29,30)

InChI key

ABXIUYMKZDZUDC-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

2-8°C

Quality Level

100

相关类别

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable purine compound that acts as a high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR) and lacks any agonist activity even at higher doses. Reportedly binds with high affinity to the ligand-binding pocket of AhR and blocks the binding of an array of exogenous and endogenous ligands. Shown to non-covalently interact with Ser317, His291, and Ser365 in human and with Ser311, His285, and Ser359 in mouse AhR. Represses AhR transcriptional activity via the dioxin response element (DRE)-dependent and independent mediated responses in human and mouse cells (IC50 = 8.5 nM in HepG2 40/6 cells).

Other Notes

Smith, K.J., et al. 2011. J. Pharmacol. Exp. Ther. 338, 318.

Packaging

Packaged under inert gas

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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