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PMSF Serine Protease Inhibidor

Cat. No.: S3025

PMSF (fluoruro de fenilmetilsulfonilo, fluoruro de bencilsulfonilo) es un inhibidor irreversible de la proteasa serina/cisteína.
PMSF  Serine Protease Inhibidor Chemical Structure

Estructura química

Peso molecular: 174.19

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.91%
99.91

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 174.19 Fórmula

C7H7FO2S

Almacenamiento (Desde la fecha de recepción)
Nº CAS 329-98-6 Descargar SDF Almacenamiento de soluciones madre

Sinónimos Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride Smiles C1=CC=C(C=C1)CS(=O)(=O)F

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 35 mg/mL (200.93 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 35 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/7518442/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9399986/
  • [6] https://pubmed.ncbi.nlm.nih.gov/10591511/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
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