PMSF

製品コードS3025 バッチS302503

化学情報

	Synonyms	Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₇H₇FO₂S
	分子量	174.19	CAS No.	329-98-6
Solubility (25°C)*	体外	DMSO	38 mg/mL (218.15 mM)
		Ethanol	38 mg/mL (218.15 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
in vitro	Although human trypsin is less susceptible to inhibition by PMSF, PMSF rapidly inactivates purified chymotrypsin from human pancreas. PMSF also rapidly inhibits acetylcholinesterase from human red cells. ^[1] As an inhibitor of phosphatidylinositol-specific phospholipase C, PMSF treatment at 2 mM almost completely inhibits carbachol-stimulated inositol incorporation into phosphatidylinositol (PI) of longitudinal smooth muscle of guinea pig ileum, while it has no effect on potassium-stimulated inositol incorporation. In contrast to its specific inhibition of carbachol-stimulated phosphoinositide turnover, PMSF produces a transient inhibition of contraction by both carbachol and potassium. ^[3] PMSF has been shown to inhibit the addition of ethanolamine phosphate to glycosylphosphatidylinositol (GPI) intermediates in Trypanosoma brucei. PMSF also inhibits the acylation of the inositol residue of GPI intermediates in bloodstream form T. brucei. PMSF inhibits ethanolamine phosphate addition and inositol acylation for procyclic forms of T. brucei but not for mammalian HeLa cells. ^[4] PMSF is the more reactive inactivator of mouse acetylcholinesterase (AChE), as the 8-fold higher BSF concentration is necessary to achieve even a 6-fold slower inactivation than that using PMSF. ^[7]
in vivo	Intraperitoneal injection of PMSF produces dose-dependent analgesia in Sprague-Dawley rats. PMSF significantly enhances the analgesic effect of beta-endorphin (END) in rats. ^[2] Mice receiving i.p. injections of PMSF exhibit cannabinoid effects that include antinociception, hypothermia and immobility with ED50 of 86 mg/kg, 224 mg/kg and 206 mg/kg, respectively. Pretreatment with an inactive dose of PMSF (30 mg/kg) enhances the effects of anandamide on tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively. ^[5] Administration of PMSF 12 hours prior to PSP causes complete protection in organophosphorus ester-induced delayed neuropathy (OPIDN) in hens, but PMSF administered 4 hours after PSP potentiates its neurotoxic effects. ^[6] Pretreatment with PMSF (30 mg/kg, i.p.) prior to an injection of 1 or 10 mg/kg 3H-anandamide results 5 minutes later in enhanced brain levels of anandamide compared to those obtained with 3H-anandamide plus vehicle injection. ^[8] Pretreatment with PMSF inhibits tri-ortho-cresyl phosphate (TOCP)-induced neurofilament (NF) degradation, and protects hens against the development of organophosphate-induced delayed neuropathy (OPIDN). ^[9] Administration of PMSF enhances the characteristic cannabimimetic effects of Δ(9)-tetrahydrocannabinol (THC) or anandamide (AEA) in ICR mice, by inhibiting the enzyme fatty acid amide hydrolase. ^[10]

プロトコル(参考用のみ)

動物実験	動物モデル	Male ICR mice subjected to anandamide injection
	投薬量	~1000 mg/kg
	投与方法	Administered i.p. 10 minutes before i.v. anandamide injection

参考

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人間や獣医の診断であるか治療的な使用のためにでない。

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