異甘草素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetIsoliquiritigeninCat. No.: HY-N0102CAS No.: 961-29-5分式: CHO分量: 256.25作靶點: Aldose Reductase; Influenza Virus; Autophagy; Apoptosis作通路: Metabolic Enzyme/Protease; Anti-infection; Autophagy; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO

2、: 100 mg/mL (390.24 mM)Ethanol : 100 mg/mL (390.24 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.9024 mL 19.5122 mL 39.0244 mL5 mM 0.7805 mL 3.9024 mL 7.8049 mL10 mM 0.3902 mL 1.9512 mL 3.9024 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，

3、避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300

4、 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.76 mM); Clear solution此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.76 mM

5、); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.76 mM); Clear solution此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL

6、作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。4. 請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.76 mM); Clear solution此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容

7、 1 mL。5. 請依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.76 mM); Clear solution此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。6. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (9.76 mM); Suspended solutio

8、n此案可獲得 2.5 mg/mL (9.76 mM，飽和度未知) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Isoliquiritigenin從光果草根中分到的黃酮類化合物，具有抗腫瘤的活性，能夠抑制 aldose reductase 的活性，IC50 值為 320 nM。Isoliquiritigenin 種流感病毒 (influenza virus) 復制的有效抑制劑，EC50 為 24.7 M。IC & Target IC50:

9、320 nM (Aldose reductase)體外研究 Isoliquiritigenin may prevent diabetic complications through inhibiting rat lens aldose reductase with an IC50 of 320nM and sorbitol accumulation in human red blood cells with an IC50 of 2.0 M1. Isoliquiritigenin (100 M) markedlyinhibits the hypoxia-induced prolonged TP

10、S and TR90 of cardiomyocytes. Isoliquiritigenin significantly triggers AMPKThr172 phosphorylation as compared with vehicle group. Isoliquiritigenin treatment also induces extracellular signal-regulated kinase (ERK) signaling pathway in the cardiomyocytes. Isoliquiritigenin treatment significantly de

11、creases theintracellular ROS levels of isolated cardiomyocytes during hypoxia/reoxygenation3. Isoliquiritigenin not onlydownregulates IL-6 expression but also significantly decreases levels of phosphorylated ERK and STAT3 and caninhibit phosphorylation levels of ERK and STAT3 induced by recombinant

12、human IL-6, which are critical signalingproteins in IL-6 signaling regulation networks4.體內(nèi)研究 Isoliquiritigenin shows concentration-dependent inhibition of the tonic contraction of mouse jejunum induced byvarious types of stimulants such as CCh (1 mM), KCl (60 mM) and BaCl2 (0.3 mM) with IC50 values

13、of 4.961.97 mM,4.031.34 mM and 3.700.58 mM, respectively2. Isoliquiritigenin exhibits significant anti-tumor activity in MMxenograft models and synergistically enhances the anti-myeloma activity of adriamycin4.戶使本產(chǎn)品發(fā)表的科研獻Page 2 of 3 www.MedChemE Am J Transl Res. 2018 Dec 15;10(12):4141-4151. Onco Ta

14、rgets Ther. 2018 Mar 22;11:1633-1642. Oncol Lett. 2018 Nov;16(5):6133-6139. Chemotherapy. 2018 Jun 22;63(3):155-161. Open Life Sci. 2017; 12: 300307See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Aida K, et al. Isoliquiritigenin: a new aldose reductase inhibitor from

15、 glycyrrhizae radix. Planta Med. 1990 Jun;56(3):254-8.2. Sato Y, et al. Isoliquiritigenin, one of the antispasmodic principles of Glycyrrhiza ularensis roots, acts in the lower part of intestine. Biol Pharm Bull. 2007Jan;30(1):145-9.3. Zhang X. Natural antioxidant-isoliquiritigenin ameliorates contr

16、actile dysfunction of hypoxic cardiomyocytes via AMPK signaling pathway. MediatorsInflamm. 2013;2013:390890.4. Chen X, et al. Isoliquiritigenin inhibits the growth of multiple myeloma via blocking IL-6 signaling. J Mol Med (Berl). 2012 Nov;90(11):1311-9.5. Traboulsi H, et al. The Flavonoid Isoliquiritigenin Reduces Lung Inflammation and Mouse Morbidity during Influenza Virus Infection. Antimicrob AgentsChemother.