苯甲基磺酰氟作用机制 - Medchemexpress - MCE中国

1、Product Data SheetPMSFCat. No.: HY-B0496CAS No.: 329-98-6分式: CHFOS分量: 174.19作靶点: Cathepsin作通路: Metabolic Enzyme/Protease储存式: Powder -20°C 3 years4°C 2 yearsIn solvent -80°C 6 months-20°C 1 month溶解性数据体外实验 DMSO : 20 mg/mL (114.82 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)

2、SolventMass1 mg 5 mg 10 mgConcentration制备储备液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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个内使，-20°C 储存时，请在 1

3、 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2 mg/mL (11.48 mM); Clear solution此案可获得 2 mg/mL (11

4、.48 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2 mg/mL (11.48 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2 mg/mL (11.48 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例

5、，取 100 L 20.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2 mg/mL (11.48 mM); Clear solution此案可获得 2 mg/mL (11.48 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 PMSF通常于制备细胞裂解物的不可

6、逆的丝氨酸/半胱氨酸蛋酶抑制剂。体外研究 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.体内研究 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.户使本产品发表的科研献 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