Eucalyptol-1-8-Cineole-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEucalyptolCat. No.: HY-N0066CAS No.: 470-82-6Synonyms: 1,8-Cineole分式: CHO分量: 154.25作靶點(diǎn): 5-HT Receptor; Potassium Channel; Interleukin Related; TNFReceptor作通路: GPCR/G Protein; Neuronal Signaling; MembraneTransporter/Ion Channel;

2、Immunology/Inflammation; Apoptosis儲(chǔ)存式: Pure form -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 : 120 mg/mL (777.96 mM)H2O : 33.33 mg/mL (216.08 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 6.4830 mL 32.4149

3、mL 64.8298 mL5 mM 1.2966 mL 6.4830 mL 12.9660 mL10 mM 0.6483 mL 3.2415 mL 6.4830 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?，配制前?qǐng)先配制澄清的儲(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

4、45% saline1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 3.5 mg/mL (22.69 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.5 mg/mL (22.69 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3.5 mg/mL (22.69 mM); Clear solutionBIOLOGICAL AC

5、TIVITY物活性 Eucalyptol是5-HT3 受體, 鉀通道, TNF- 和 IL-1 的抑制劑。IC50 & Target 5-HT3 Receptor IL-1 TNF- potassium channel體外研究 Eucalyptol inhibits 5-HT-evoked currents in oocytes expressing 5-HT3 receptors with an IC50 of 258 M 1.Eucalyptol (Cin) treatment significantly decreases the ROS level in A25-35 treated

6、cells in a dosedependent manner. Eucalyptol treatment significantly decreases the NO level in A25-35 treated cells in adose dependent manner (p25-35 treated cells in a dose dependent manner (p25-35 treated PC12 cells. IL-6level is also attenuated by Eucalyptol in dose dependent manner (p25-35 treate

7、d cells 3.體內(nèi)研究 Results show that male and female rats treated with Eucalyptol (CIN) at the highest doses, 500 and 1000mg/kg, have shown lower body weight than control group from the 7th to 50th day of treatment. Theadministration of Eucalyptol significantly reduces body weight gain of male rats (Euc

8、alyptol 500 and 1000mg/kg) and female rats (Eucalyptol 1000 mg/kg) in the first week of treatment. However, this reduction isfollowed by an increase in body weight of rats males and females treated with all doses of the second weekuntil the end of treatment. For male rats, there is a significant inc

9、rease of 6.93% in mean corpuscular volume(MCV) (Eucalyptol 1000 mg/kg) and of 43.54 and 38.98% in the platelet count (Eucalyptol 500 and 1000mg/kg, respectively) and a decrease of 6.74 and 6.67% in mean corpuscular hemoglobin concentration(MCHC) (Eucalyptol 500 and 1000 mg/kg) and mean platelet volu

10、me (MPV) of 10.40, 10.60 and 15.73%(Eucalyptol 100, 500 and 1000 mg/kg, respectively), when compare to the control group 4.PROTOCOLCell Assay 3 The protective dose of Eucalyptol (Cineole) is determined by MTT dye-uptake method. In brief, cells (1104per well) are seeded in 96-well tissue culture plat

11、es and allowed to adhere for 24 h in CO2 incubator at 37C.Cells are differentiated for the indicated time period. Thereafter, the medium is replaced with the mediumcontaining Eucalyptol (0 to 10 M) in different experiments for a period up to 24 h. Tetrazolium bromide salt(5 mg/mL of stock in PBS) 10

12、 L/well is added in 100 mL of cell suspension and plate is incubated for 4 h. Atthe end of incubation period, the reaction mixture is carefully taken out and 200 L of DMSO is added toeach well by pipetting up and down several times until the content gets homogenized. The plates are kept onrocker sha

13、ker for 10 min at room temperature and then read at 550 nm using microplate reader 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Swiss mice are used in this experiment. The animals are randomly divided into two groups (n=5) and fasted2/3 Mast

14、er of Small Molecules 您邊的抑制劑師www.MedChemEAdministration 4 overnight with free access to water. The group control receives a 1% Tween-80 aqueous solution (0.1 mL/10g) and the other group is treated with Eucalyptol a single 2000 mg/kg dose by oral route. The animals areobserved at 30, 60, 120, 180 and

15、 240 min after oral treatment and daily for 14 days. Behavioral changes,weight, food and water consumption, clinical signs of toxicity or mortality are recorded daily 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jarvis GE, et al. Nonco

16、mpetitive Inhibition of 5-HT3 Receptors by Citral, Linalool, and Eucalyptol Revealed by Nonlinear Mixed-EffectsModeling. J Pharmacol Exp Ther. 2016 Mar;356(3):549-62.2. Zeraatpisheh Z, et al. Eucalyptol induces hyperexcitability and epileptiform activity in snail neurons by inhibiting potassium chan

17、nels. EurJ Pharmacol. 2015 Oct 5;764:70-8.3. Khan A, et al. 1,8-cineole (eucalyptol) mitigates inflammation in amyloid Beta toxicated PC12 cells: relevance to Alzheimers disease.Neurochem Res. 2014 Feb;39(2):344-52.34. Caldas GF, et al. Repeated-doses and reproductive toxicity studies of the monoterpene 1,8-cineole (eucalypto