182707

GNF351

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

• Synonyma: 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
• Empirický vzorec (Hillův zápis): C₂₄H₂₅N₇
• Číslo CAS: 1227634-69-6
• Molekulová hmotnost: 411.50
• MDL number: MFCD23726597
• UNSPSC Code: 12352200
• NACRES: NA.77

Vlastnosti

• Název produktu: 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).
• Quality Level: 100
• 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
• 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

Popis

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Bezpečnostní informace

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable