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PMSF
別名：Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride
PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
CAS No. 329-98-6
文献中Selleckの製品使用例（23）
製品安全説明書
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純度：
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PMSF 関連製品
| 関連化合物ライブラリー | FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library | もっと見る |
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Serine Protease阻害剤の選択性比較
生物活性
| 製品説明 | PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. | ||
|---|---|---|---|
| Targets |
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| In Vitro | ||||
| 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 | ||
| 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] | |
|---|---|---|
| 動物実験 | 動物モデル | Male ICR mice subjected to anandamide injection |
| 投与量 | ~1000 mg/kg | |
| 投与経路 | Administered i.p. 10 minutes before i.v. anandamide injection | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04062786 | Unknown status | Scheduled Heart Surgery|Valve Replacement|Coronary Artery Bypass |
University Hospital Strasbourg France |
February 21 2019 | -- |
| NCT03300323 | Unknown status | Peri-operative Fluid Management |
St George''s Healthcare NHS Trust |
October 2017 | Not Applicable |
| NCT02569008 | Completed | Post Cardiac Surgery |
St George''s University of London |
January 2014 | Not Applicable |
化学情報
| 分子量 | 174.19 | 化学式 | C7H7FO2S |
| CAS No. | 329-98-6 | SDF | Download PMSF SDFをダウンロードする |
| Smiles | C1=CC=C(C=C1)CS(=O)(=O)F | ||
| 保管 | |||
|
In vitro |
DMSO : 35 mg/mL ( (200.93 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 35 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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