Dihydrotanshinone-I _Quinone - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDihydrotanshinone ICat. No.: HY-N0360CAS No.: 87205-99-0分式: CHO分量: 278.3作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 4.76 mg/mL (17.10 mM; Need ultrasonic)Mass Solv

2、ent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.5932 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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂

3、在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.48 mg/mL (1.72 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.48 mg/mL (1.72 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.48 mg/mL (1.72

4、mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Dihydrotanshinone I从丹参中分离到的天然产物，泛于管疾病的治疗。体外研究 In lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs), DHT (10 nM)decreases lectin-like ox-LDL receptor-1 (LOX-1) and NADPH oxidas

5、e 4 (NOX4) expression, reactive oxygenspecies (ROS) production, NF-B nuclear translocation, ox-LDL endocytosis and monocytes adhesion 1.Dihydrotanshinone I induces caspase dependent apoptosis induced in HCT116 cells. Dihydrotanshinone Iinduces concentration and ROS dependent caspase activation. Apop

6、tosis induced by Dihydrotanshinone I iscompletely prevented by Z-VAD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly inhibited bypretreatment of Z-LEHD-fmk but only is partially inhibited by Z-IETD-fmk. Apoptosis induced byDihydrotanshinone I is significantly increased by caspase-2 kn

7、ockdown 3.体内研究 DHT (10 and 25 mg/kg) significantly attenuates atherosclerotic plaque formation, alteres serum lipid profile,decreases oxidative stress and shrinks necrotic core areas in ApoE-/- mice. DHT dramatically inhibits theenhanced expression of LOX-1, NOX4, and NF-B in aorta 1. Dihydrotanshin

8、one I (1, 2, 4 mg/kg) treatmentcan improve cardiac function, reduce infarct size, ameliorate the variations in myocardial zymogram andhistopathological disorders, decrease 20-HETE generation, and regulate apoptosis-related protein inmyocardial ischemia-reperfusion rats 2.PROTOCOLKinase Assay 3 Cells

9、 are treated with various concentrations of Dihydrotanshinone I (3.13-20 M) for 48 h. For the activityassay, Ac-DEVD-AMC (1 g/L), Ac-IETD-AMC (1 g/L) or Ac-LEDH-AMC (1 g/L) and cell lysate areadded into Protease Assay Buffer in 96-well plate. Reaction mixtures with lysis buffer are used as negativec

10、ontrols. Cells treated with DMSO (0.1%) are treated as vehicle control. The reaction mixtures are incubatedfor 1 h at 37C. The AMC liberated from the substrates is measured using spectrofluorometer of Victor 2plate reader with an excitation wavelength of 380 nm and an emission wavelength of 430 nm.M

11、CE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male ApoE-/- mice (6-8 weeks old) on C57BL/6J background and age-matched wild-type C57BL/6J controlsAdministration 1 housed in SPF-grade animal facilities with a 12 h light/dark cycle, at 23C (2C). S

12、tarting from 6 weeks, themice are fed with a HCD (54.35% raw grain, 20% lard, 0.15% cholesterol, 15% sucrose, 0.5% SodiumCholate, 10% yolk powder) for 12 weeks. All ApoE-/- mice are dosed daily via intragastric gavage with 10and 25 mg/kg Dihydrotanshinone I dissolved in 0.5% CMC-Na or administered 0

13、.5% CMC-Na alone (vehiclecontrol) (n=8 per group).MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhao W, et al. Dihydrotanshinone I Attenuates Atherosclerosis in ApoE-Deficient Mice: Role of NOX4/NF-B Mediated Lectin-LikeOxidized LDL Recep

14、tor-1 (LOX-1) of the Endothelium. Front Pharmacol. 2016 Nov 8;7:418. eCollection 2016.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 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 Nov