二氫丹參酮 I作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetDihydrotanshinone ICat. No.: HY-N0360CAS No.: 87205-99-0分式: CHO分量: 278.3作靶點(diǎn): SARS-CoV作通路: 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 : 4.76 mg/mL (17.10 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.59

2、32 mL 17.9662 mL 35.9324 mL5 mM 0.7186 mL 3.5932 mL 7.1865 mL10 mM 0.3593 mL 1.7966 mL 3.5932 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。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?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的

3、可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.48 mg/mL (1.72 mM); Suspended solution; Need ultrasonic此案可獲得 0.48 mg/mL (1.72 mM) 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 4.7999

4、997 mg/mL 的澄清DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.48 mg/mL (1.72 mM); Clear solution此案可獲得 0.48 mg/mL (1.72 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 4.7999997 mg/mL 的澄，混合均勻。DMS

5、O 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.48 mg/mL (1.72 mM); Clear solution此案可獲得 0.48 mg/mL (1.72 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 4.7999997 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Dihydrotanshinone I CoV。從丹參中分離到的天然產(chǎn)物，泛于管

6、疾病的治療。Dihydrotanshinone I 可抑制 MERS-體外研究 In lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs), DHT (10 nM) decreaseslectin-like ox-LDL receptor-1 (LOX-1) and NADPH oxidase 4 (NOX4) expression, reactive oxygen species (ROS)production, NF-B nuclear translocation, ox-LD

7、L endocytosis and monocytes adhesion1. Dihydrotanshinone Iinduces caspase dependent apoptosis induced in HCT116 cells. Dihydrotanshinone I induces concentration and ROSdependent caspase activation. Apoptosis induced by Dihydrotanshinone I is completely prevented by Z-VAD-fmk.Apoptosis induced by Dih

8、ydrotanshinone I is significantly inhibited by pretreatment of Z-LEHD-fmk but only ispartially inhibited by Z-IETD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly increased by caspase-2knockdown3.體內(nèi)研究 DHT (10 and 25 mg/kg) significantly attenuates atherosclerotic plaque formation, alt

9、eres serum lipid profile,decreases oxidative stress and shrinks necrotic core areas in ApoE-/- mice. DHT dramatically inhibits the enhancedexpression of LOX-1, NOX4, and NF-B in aorta1. Dihydrotanshinone I (1, 2, 4 mg/kg) treatment can improve cardiacfunction, reduce infarct size, ameliorate the var

10、iations in myocardial zymogram and histopathological disorders,decrease 20-HETE generation, and regulate apoptosis-related protein in myocardial ischemia-reperfusion rats2.PROTOCOLKinase Assay 3 Cells are treated with various concentrations of Dihydrotanshinone I (3.13-20 M) for 48 h. For the activi

11、ty assay, Ac-DEVD-AMC (1 g/L), Ac-IETD-AMC (1 g/L) or Ac-LEDH-AMC (1 g/L) and cell lysate are added into ProteaseAssay Buffer in 96-well plate. Reaction mixtures with lysis buffer are used as negative controls. Cells treated withDMSO (0.1%) are treated as vehicle control. The reaction mixtures are i

12、ncubated for 1 h at 37C. The AMC liberatedfrom the substrates is measured using spectrofluorometer of Victor 2 plate reader with an excitation wavelength of380 nm and an emission wavelength of 430 nm.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Anima

13、l Male ApoE-/- mice (6-8 weeks old) on C57BL/6J background and age-matched wild-type C57BL/6J controls housed inAdministration 1 SPF-grade animal facilities with a 12 h light/dark cycle, at 23C (2C). Starting from 6 weeks, the mice are fed with aHCD (54.35% raw grain, 20% lard, 0.15% cholesterol, 15

14、% sucrose, 0.5% Sodium Cholate, 10% yolk powder) for 12weeks. All ApoE-/- mice are dosed daily via intragastric gavage with 10 and 25 mg/kg Dihydrotanshinone I dissolvedin 0.5% CMC-Na or administered 0.5% CMC-Na alone (vehicle control) (n=8 per group).MCE has not independently confirmed the accuracy

15、 of these methods. They are for reference only.REFERENCESPage 2 of 3 www.MedChemE1. Zhao W, et al. Dihydrotanshinone I Attenuates Atherosclerosis in ApoE-Deficient Mice: Role of NOX4/NF-B Mediated Lectin-Like Oxidized LDLReceptor-1 (LOX-1) of the Endothelium. Front Pharmacol. 2016 Nov 8;7:418. eColl

16、ection 2016.2. Wei Y, et al. The cardioprotection of dihydrotanshinone I against myocardial ischemia-reperfusion injury via inhibition of arachidonic acid -hydroxylase.Can J Physiol Pharmacol. 2016 Dec;94(12):1267-1275. Epub 2016 Jun 24.3. Wang L, et al. Dihydrotanshinone I induced apoptosis and autophagy through caspase dependent pathway in colon cancer. Phytomedicine. 2015 Nov15;22(12):1079-874. Ji Yeun Kim, et al. Safe, High-Throughput Screening of Natural Compounds of MERS-CoV Entry Inhibitors Using a Pseudovirus Expressing MERS-CoVSpike Protein. Int J Antimicro