1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEForsythoside BCat. No.: HY-N0029CAS No.: 81525-13-5分式: CHO分量: 756.7作靶點: TNF Receptor; NF-B作通路: Apoptosis; NF-B儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 125 mg/mL (165.19 mM; Need ultr

2、asonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.3215 mL 6.6076 mL 13.2153 mL5 mM 0.2643 mL 1.3215 mL 2.6431 mL10 mM 0.1322 mL 0.6608 mL 1.3215 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，適當保

3、存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (2.75 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (2.75 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (2.75 mM); C

4、lear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Forsythoside B傳統中藥植物獨味的葉中分離的苯醇苷。獨味可于治療炎癥疾病和促進液循環。Forsythoside B 可抑制 TNF-alpha，IL-6，IB， 調節 NF-B。IC50 & Target NF-B TNF-體外研究 Forsythoside B concentration-dependently down-regulates the levels of TNF-, IL-6 and high-mo

5、bility group-box1 protein (HMGB1) in lipopolysaccharide (LPS)-stimulated RAW264.7 cells, inhibits the IB kinase (IKK)pathway and modulated nuclear factor (NF)- B 1.體內研究 Intravenous injection of forsythoside B alone or plus imipenem reduces serum levels of TNF-, IL-6, HMGB1,triggering receptor expres

6、sed on myeloid cells (TREM-1) and endotoxin, while the serum level of IL-10 is up-regulated and myeloperoxidase (MPO) in lung, liver and small intestine is reduced 1. Forsythoside B atdoses higher than 8 mg/kg produces a significant neuroprotective potential in cerebral ischemia andreperfusion rats.

7、 Forsythoside B (20 mg/kg) demonstrates significant neuroprotective activity even afterdelayed administration at 1 h, 3 h and 5 h after cerebral ischemia and reperfusion. Forsythoside B 20 mg/kgattenuates histopathological damage as demonstrated by smaller brain infarct size and brain edema,decrease

8、d cerebral Evans blue extravasation and myeloperoxidase activity, inhibited cerebral phosphor-IB- and NF-B expression 2. Forsythoside B shows a significant recovery in myocardial function withimprovement of LVSP and +/-dp/dt(max). The myocardial infarct volume, serum levels of Tn-T, TNF-alphaand IL-

9、6, content of MDA and MPO activity in myocardial tissue are all reduced, protein expression ofHMGB1, phosphor-I kappaB-alpha and phosphor-NF-kappaB are down-regulated, while attenuate thedecrease of SOD and GPx activities 3.PROTOCOLCell Assay 1 Forsythoside B is dissolved in sterile saline solution

10、and added to the medium at various concentrations(from 0.1 to 10 M) and incubated with LPS stimulated RAW264.7 cells. Cell-free supernatants are collectedafter Forsythoside B treatment for 24 h. Cell viability is assessed by measuring lactate dehydrogenase (LDH)in the medium 1.MCE has not independen

11、tly confirmed the accuracy of these methods. They are for reference only.Animal Rats: Forsythoside B is dissolved in sterilized saline. For the doseresponse study, forsythoside B at dosesAdministration 2 of 1.3, 3.2, 8, 20 or 50 mg/kg is administered as an intravenous bolus injection at 15 min after

12、 reperfusion.The sham or vehicle-treated rats are injected with saline. Neurological deficits are determined at 23 h afterreperfusion followed by brain infarct volume examination 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jiang WL, e

13、t al. Forsythoside B protects against experimental sepsis by modulating inflammatory factors. Phytother Res. 20122/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEJul;26(7):981-7.2. Jiang WL, et al. Neuroprotective efficacy and therapeutic window of Forsythoside B: in a rat model of cerebral ischemia and reperfusioninjury. Eur J Pharmacol. 2010 Aug 25;640(1-3):75-81.3. Jiang WL, et al. Cardioprotection with forsythoside B in rat myocardial ischemia-reperfusion injury: relation to inflammation response.Phytomedicine. 2010 Jul;17(8-9):6