苯甲基磺酰氟作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetPMSFCat. No.: HY-B0496CAS No.: 329-98-6分式: CHFOS分量: 174.19作靶點(diǎn): Cathepsin作通路: Metabolic Enzyme/Protease儲存式: Powder -20°C 3 years4°C 2 yearsIn solvent -80°C 6 months-20°C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 20 mg/mL (114.82 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)

2、SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 5.7409 mL 28.7043 mL 57.4086 mL5 mM 1.1482 mL 5.7409 mL 11.4817 mL10 mM 0.5741 mL 2.8704 mL 5.7409 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請?jiān)?6 個內(nèi)使，-20°C 儲存時，請?jiān)?1

3、 個內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2 mg/mL (11.48 mM); Clear solution此案可獲得 2 mg/mL (11

4、.48 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.0 mg/mL 的澄 DMSO 儲備液加到 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. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2 mg/mL (11.48 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2 mg/mL (11.48 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例

5、，取 100 L 20.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2 mg/mL (11.48 mM); Clear solution此案可獲得 2 mg/mL (11.48 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 PMSF通常于制備細(xì)胞裂解物的不可

6、逆的絲氨酸/半胱氨酸蛋酶抑制劑。體外研究 PMSF (2 mM) inhibits carbachol-stimulated inositol phosphate accumulation in the presence of Li+ by only 15%-19%.PMSF inhibition of phosphoinositide turnover is due to one or more steps following phosphoinositide breakdown1.PMSF inhibits the acylation of the inositol residue of

7、GPI intermediates in bloodstream form T. brucei. PMSF inhihitsthe formntion of glycolipid C but does not inhibit fatty acid remodeling in vitro. PMSF inhihits GPI acylation andethanolamine phosphatp addition in procyclic trypanosomes but not in Hela cells2.體內(nèi)研究 PMSF (0.1 mL/10 g b.wt, i.p.) produces

8、 antinociception as indicated by the dose-responsive increase in % MPE in thetail-flick latency evaluation, but fails to produce a clear dose-responsive inhibition of locomotion. Mice receiving i.p. injections of PMSF exhibit cannabinoid effects that includes antinociception, hypothermia and immobil

9、ity with ED50values of 86, 224 and 206 mg/kg, respectively. PMSF (30 mg/kg) pretreatment potentiates the effects of anandamideon tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively3.PROTOCOLAnimal Male ICR mice weighing 18 to 25 g are used in

10、the assay. PMSF is dissolved in sesame oil and administered i.p. at aAdministration 3 volume of 0.1 mL/10 g b.wt. PMSF is always administered 10 min before i.v. anandamide or vehicle injections. Miceare acclimated to the evaluation room overnight without interruption of food or water. After i.v. ana

11、ndamide orvehicle administration each animal is evaluated as follows: tail-flick latency (antinociception) response at 5 min andspontaneous (locomotor) activity at 5 to 15 min; or core (rectal) temperature at 5 min and ring-immobility (catalepsy)at 5 to 10 min.MCE has not independently confirmed the

12、 accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Physiol Biochem. 2017;44(3):1051-1063. J Cell Physiol. 2019 Dec;234(12):22960-22971. Mol Cancer Res. 2020 Feb;18(2):204-215. J Pharmacol Exp Ther. 2019 Jul;370(1):62-71. Int Immunopharmacol. 2019 Jan 30;69:143-149.See more cust

13、omer validations on www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Sekar, M.C. and B.D. Roufogalis, Differential effects of phenylmethanesulfonyl fluoride (PMSF) on carbachol and potassium stimulated phosphoinositideturnover and contraction in longitudinal smooth muscle of guinea pig ileum. Cell C

14、alcium, 1984. 5(3): p.2. Guther, M.L., W.J. Masterson, and M.A. Ferguson, The effects of phenylmethylsulfonyl fluoride on inositol-acylation and fatty acid remodeling in Africantrypanosomes. J Biol Chem, 1994. 269(28): p. 18694-701.3. Compton, D.R. and B.R. Martin, The effect of the enzyme inhibitor phenylmethylsulfonyl fluoride on the pharmacological effect of anandamide in themouse model of cannabimimetic activity. J Pharmacol Exp Ther, 1997. 283(3): p. 1138-43.Mce