SC75741 - NF-κB 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESC75741Cat. No.: HY-10496CAS No.: 913822-46-5分式: CHNOS分量: 565.67作靶點(diǎn): NF-B; Caspase; Influenza Virus作通路: NF-B; Apoptosis; Anti-infection儲(chǔ)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(shí)驗(yàn) DMSO : 125 mg

2、/mL (220.98 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7678 mL 8.8391 mL 17.6782 mL5 mM 0.3536 mL 1.7678 mL 3.5356 mL10 mM 0.1768 mL 0.8839 mL 1.7678 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保

3、證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.68 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.68 mM); Suspended solution; Need ultrasonic3.

4、 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (3.68 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SC75741泛，有效的 NF-B 抑制劑，對(duì) p65 的 IC50 為 200 nM。SC75741 以毒濃度阻斷流感病毒 (IV)復(fù)制。SC75741 先損害 NF-B 亞 p65 的 DNA 結(jié)合，導(dǎo)致細(xì)胞因，趨化因和促凋亡因的表達(dá)降低，隨后抑制 caspase 活化和阻斷 caspas

5、e 介導(dǎo)的病毒核糖核蛋 (viralribonucleoproteins) 的核輸出。IC50 & Target p65 Caspase200 nM (IC50)體外研究 SC75741 (5 M; 24-96 hours) inhibits long-term A549 cells proliferation 2.SC75741 (1-10 M; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent mannerindicating a cytostatic effect for A549 cells

6、within a time frame of about 50 and 65hours 2.SC75741 (5 M; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection2.Cell Proliferation Assay 2Cell Line: A549 cellsConcentration: 5MIncubation Time: 24, 48, 72 and 96hoursResult: Inhibited long-term cell proliferatio

7、nCell Viability Assay 2Cell Line: A549 cellsConcentration: 1, 2, 5 or 10MIncubation Time: 5.5, 29, 50, 65 hoursResult: Reduced cells viability in a concentration-dependent manner.Western Blot Analysis 2Cell Line: MDCK cellsConcentration: 5MIncubation Time: 24 hoursResult: Inhibited cleavage of the e

8、ffector caspase 3 induced upon H7N7-infection.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 SC75741 (intraperitoneal injection; 15mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virusmRNA by 90% in the lungs of infected mice 2.The plasma-levels of SC74751 (intravenously of 5 mg

9、/kg and intraperitoneally of 15 mg/kg; for 3.5 and 6hours) after i.v. administration decreases mono-exponentially and half-life is roughly 40 min. After i.p.administration, elimination of SC75741 seems to be limited by a slow uptake from the peritoneum and a half-life of 55 min is observed 1.Animal

10、Model: Inbred female C57BL/6 mice at the age of 6-8 weeks 2Dosage: 15mg/kgAdministration: Intraperitoneal injection; for 2 daysResult: Reduced the amount of viral mRNA by 90%.Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks 1Dosage: 5 mg/kg or 15 mg/kgAdministration: Intravenously of

11、 5 mg/kg and intraperitoneally of 15 mg/kg; 3.5 and 6 hoursResult: Half-life was roughly 40 min and 55 min for i.v. and i.p. administration, respectively.REFERENCES1. Haasbach E, et al. The NF-kappaB inhibitor SC75741 protects mice against highly pathogenic avian influenza A virus. Antiviral Res.2013 Sep;99(3):336-44.2. Ehrhardt C, et al. The NF-B inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for developmentof viral resistance. Cell Microbiol. 2013 Jul;15(7):1198-211.McePdfHeightCaution: Produ