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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOxythiamineCat. No.: HY-107430CAS No.: 136-16-3Synonyms: Hydroxythiamin分式: CHNOS分量: 266.34作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 51.67 mg/mL (194.00 mM; Need ultrasonic
2、)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.7546 mL 18.7730 mL 37.5460 mL5 mM 0.7509 mL 3.7546 mL 7.5092 mL10 mM 0.3755 mL 1.8773 mL 3.7546 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
3、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: 2.58 mg/mL (9.69 mM); Clear solution2. 請(qǐng)依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (9.69 mM); Clear solution3. 請(qǐng)依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (9.69 mM); Clear
4、solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Oxythiamine種抗代謝物和維素B1 (vitamin B1)拮抗劑,也是眾所周 知的硫銨 (thiamine) 拮抗劑和轉(zhuǎn)酮醇酶 (transketolase) 抑制劑。IC50 & Target Vitamin B1, Thiamine, Transketolase 1.體外研究 Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-know
5、n thiamine antagonist andinhibitor of transketolase. Oxythiamine alters protein expression in a dose dependent manner. The level ofalpha-enolase is increased by Oxythiamine treatment, while expression of 14-3-3 protein beta/alpha issuppressed by Oxythiamine at a stratified dose. Oxythiamine causes d
6、ynamic changes of total proteinexpression in time dependent fashion. Oxythiamine suppresses expression of cellular phosphor proteinssignificantly 2.PROTOCOLCell Assay 2 Human pancreatic carcinoma cell line MIA PaCa-2 is used throughout the study. Experiments are set up intwo groups: dose and time-de
7、pendent groups. For the dose-dependent group, the cells are stimulated with 5,50 and 500 M Oxythiamine (OT) for 48 hours, respectively. The unstimulated cells are considered ascontrol. For the time-dependent group, the cells are stimulated with 50 M Oxythiamine in MEM containingnatural amino acids o
8、r 50% of 15 N algal amino acid mixture for 12 and 48 h. The unstimulated cells areconsidered as the zero time point. Each treatment is repeated four times with 10 mL/flask. The cell pelletsare then collected for further analysis 2.MCE has not independently confirmed the accuracy of these methods. Th
9、ey are for reference only.REFERENCES1. Moradi H, et al. Functional thiamine deficiency in end-stage renal disease: malnutrition despite ample nutrients. Kidney Int. 2016Aug;90(2):252-254.2. Wang J, et al. Inhibition of transketolase by oxythiamine altered dynamics of protein signals in pancreatic cancer cells. Exp HematolOncol. 2013 Jul 27;2:18.McePdfHeightCaution: Product has not been fully validated for med
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