Sofalcone

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Chemical Structure| 64506-49-6 同义名 : Solon; SU 88; RTECS AJ7126000.; Isoprenyl chalcone; BRN 2191482
CAS号 : 64506-49-6
货号 : A278552
分子式 : C27H30O6
纯度 : 97%
分子量 : 450.52
MDL号 : MFCD00868207
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
生物活性
描述 Sofalcone, a gastric antiulcer agent, is known to induce the expression of Heme oxygenase-1 (HO-1) in gastric epithelium. Sofalcone potently increased HO-1 mRNA and protein in both primary trophoblasts and human umbilical vein endothelial cells. Furthermore, sofalcone treatment caused nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 and transactivation of other nuclear factor (erythroid-derived 2)-like 2 responsive genes (NQO1, TXN, and GCLC). Importantly, sofalcone significantly decreased the secretion of sFlt-1 from primary human trophoblasts[2]. Sofalcone activated the Nrf2-HO-1 pathway by covalently binding to KEAP1 via Michael addition, and may confer anti-colitic effects by inducing Nrf2 activation[3]. Sofalcone promoted gastric ulcer healing during 7 weeks of treatment following 1 week of eradication therapy, and the healing rate was equivalent to that of cimetidine. Symptom disappearance rates were significantly better in the sofalcone group than in the cimetidine group[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL

参考文献

[2]Onda K, Tong S, Nakahara A, Kondo M, Monchusho H, Hirano T, Kaitu'u-Lino T, Beard S, Binder N, Tuohey L, Brownfoot F, Hannan NJ. Sofalcone upregulates the nuclear factor (erythroid-derived 2)-like 2/heme oxygenase-1 pathway, reduces soluble fms-like tyrosine kinase-1, and quenches endothelial dysfunction: potential therapeutic for preeclampsia. Hypertension. 2015 Apr;65(4):855-62

[3]Kim W, Lee H, Kim S, Joo S, Jeong S, Yoo JW, Jung Y. Sofalcone, a gastroprotective drug, covalently binds to KEAP1 to activate Nrf2 resulting in anti-colitic activity. Eur J Pharmacol. 2019 Dec 15;865:172722

[4]Higuchi K, Watanabe T, Tanigawa T, Tominaga K, Fujiwara Y, Arakawa T. Sofalcone, a gastroprotective drug, promotes gastric ulcer healing following eradication therapy for Helicobacter pylori: a randomized controlled comparative trial with cimetidine, an H2-receptor antagonist. J Gastroenterol Hepatol. 2010 May;25 Suppl 1:S155-60