摘要：GNF351是一种芳基烃受体(AHR)拮抗剂，GNF351与光亲和性AHR配体竞争结合到AHR的IC50值为62 nM。

生物活性

GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 (500 nM, 48 hours) significantly reduces the percentage of Ki67-positive cells and cell number after treating proliferating monolayer cultures of human keratinocytes.

化学性质

分子量 411.5

分子式 C24H25N7

溶解性（25°C） DMSO ≥ 90 mg/mL

储存条件 粉末型式 -20°C 3年；4°C 2年

溶于溶剂 -80°C 6个月；-20°C 1个月

运输方式 冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg

1 mM 2.4301 mL 12.1507 mL 24.3013 mL

5 mM 0.486 mL 2.4301 mL 4.8603 mL

10 mM 0.243 mL 1.2151 mL 2.4301 mL

参考文献

[1] Shusuke Ozawa, et al. Life Sci. Expression profile of cytochrome P450s and effects of polycyclic aromatic hydrocarbons and antiepileptic гυgs on CYP1 expression in MOG-G-CCM cells

[2] Ellen H van den Bogaard, et al. J Invest Dermatol. Genetic and pharmacological analysis identifies a physiological role for the AHR in epidermal differentiation

[3] Tejas S Lahoti, et al. Ann Rheum Dis. Aryl hydrocarbon receptor antagonism mitigates cytokine-mediated inflammatory signalling in primary human fibroblast-like synoviocytes

来源：AbMole