Name: PMSF
Brand: Selleck Chemicals
SKU: S3025
Rating: 5 (25 reviews)

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.91%

99.91

Cibles apparentées	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP
Autre Serine Protease Inhibiteurs	Leupeptin Hemisulfate Nafamostat mesilate (FUT-175) AEBSF HCl Alvelestat (AZD9668) Gabexate Mesylate Sivelestat sodium tetrahydrate Sivelestat sodium UK-371804 HCl Fulacimstat ZK824859

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	174.19	Formule	C₇H₇FO₂S	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	329-98-6	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride			Smiles	C1=CC=C(C=C1)CS(=O)(=O)F

Solubilité (Solubility)

In vitro
Lot:

DMSO : 35 mg/mL (200.93 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 35 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	1.750mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 35 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	1.750mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 35 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC₅₀/Ki	cysteine protease chymotrypsin
In vitro	Although human trypsin is less susceptible to inhibition by PMSF, this compound rapidly inactivates purified chymotrypsin from human pancreas. It also rapidly inhibits acetylcholinesterase from human red cells. As an inhibitor of phosphatidylinositol-specific phospholipase C, treatment with this chemical 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, this agent produces a transient inhibition of contraction by both carbachol and potassium. It has been shown to inhibit the addition of ethanolamine phosphate to glycosylphosphatidylinositol (GPI) intermediates in Trypanosoma brucei. This inhibitor also inhibits the acylation of the inositol residue of GPI intermediates in bloodstream form T. brucei. It inhibits ethanolamine phosphate addition and inositol acylation for procyclic forms of T. brucei but not for mammalian HeLa cells. This compound 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.
In vivo	Intraperitoneal injection of PMSF produces dose-dependent analgesia in Sprague-Dawley rats. This compound significantly enhances the analgesic effect of beta-endorphin (END) in rats. Mice receiving i.p. injections of this chemical 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 this compound (30 mg/kg) enhances the effects of anandamide on tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively. Administration of this chemical 12 hours prior to PSP causes complete protection in organophosphorus ester-induced delayed neuropathy (OPIDN) in hens, but it administered 4 hours after PSP potentiates its neurotoxic effects. Pretreatment with this compound (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. Pretreatment with it inhibits tri-ortho-cresyl phosphate (TOCP)-induced neurofilament (NF) degradation, and protects hens against the development of organophosphate-induced delayed neuropathy (OPIDN). Administration of this chemical enhances the characteristic cannabimimetic effects of Δ(9)-tetrahydrocannabinol (THC) or anandamide (AEA) in ICR mice, by inhibiting the enzyme fatty acid amide hydrolase.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/4306345/ [2] https://pubmed.ncbi.nlm.nih.gov/6292607/ [3] https://pubmed.ncbi.nlm.nih.gov/6090026/ [4] https://pubmed.ncbi.nlm.nih.gov/7518442/ [5] https://pubmed.ncbi.nlm.nih.gov/9399986/ [6] https://pubmed.ncbi.nlm.nih.gov/10591511/

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

PMSF Serine Protease Inhibiteur

Poids moléculaire: 174.19