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Doxycycline Hyclate MMP inhibitor

Cat. No.: S4163

Doxycycline Hyclate is a member of the tetracycline antibiotics group, and is commonly used to treat a variety of infections. It is also an inhibitor of matrix metallo-proteinases (MMP).
Doxycycline Hyclate Antineoplastic and Immunosuppressive Antibiotics inhibitor Chemical Structure

Estructura química

Peso molecular: 512.94

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.87%
99.87

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
SW1353 Function assay 50 uM Inhibition of IL-1-beta-induced MMP13 production in human SW1353 cells at 50 uM 17267227
K-12 BW25113 Bactericidal assay 24 hrs Bactericidal activity against yafQ gene-deficient Escherichia coli K-12 BW25113 biofilm assessed as log reduction of viable cells after 24 hrs 19307375
K-12 BW25113 Bactericidal assay 24 hrs Bactericidal activity against Escherichia coli K-12 BW25113 biofilm harboring pCA24N ptac::yafQ plasmid assessed as log reduction of viable cells after 24 hrs pretreated with 5 uM of IPTG for 4 hrs 19307375
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 15 μM. 19482476
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 20 μM. 19482476
THP1 Function assay Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Plasmodium falciparum, IC50 = 3.1 μM. 19748781
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells after 72 hrs by propidium iodide staining-based flow cytometry, IC50 = 20 μM. 19748781
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 15 μM. 19926173
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 20 μM. 19926173
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 20 μM. 21741131
Neuro2a Function assay 1 uM Decrease in 7-DHC levels in Dhcr7-deficient mouse Neuro2a cells at 1 uM by LC-MS/GC-MS analysis 26789657
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells measured after 72 hrs by MTT assay, CC50 = 20 μM. 27155463
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, CC50 = 20 μM. 27654395
CD Antibacterial assay 25 ug/ml 72 hrs Antibacterial activity against Rickettsia prowazekii str. Breinl infected in CD rat primary pulmonary vascular endothelial cells assessed as bacterial shape change at 25 ug/ml measured 72 hrs post infection by Hoechst 33258/phalloidin staining based fluor 28089350
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
skeletal myoblast cells Cytotoxicity assay DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50 = 14.49 μM. ChEMBL
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 512.94 Fórmula

C22H24N2O8.1/2C2H6O.HCl.1/2H2O

Almacenamiento (Desde la fecha de recepción)
Nº CAS 24390-14-5 Descargar SDF Almacenamiento de soluciones madre

Sinónimos WC2031 Smiles CCO.CC1C2C(C3C(C(=O)C(=C(C3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.CC1C2C(C3C(C(=O)C(=C(C3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.O.Cl.Cl

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (194.95 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 100 mg/mL

Ethanol : 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
MMP
In vitro

Doxycycline hyclate 10% (DOXY) has significant toxicity effects on osteoblast cells compared to the control group with a mean cell viability of 84%. Doxycycline hyclate 10% (DOXY) results in a significantly higher alkaline phosphatase activity (approximately 56%) than the control in osteoblasts. Doxycycline hyclate 10% (DOXY) seems to slightly altered the morphology of the osteoblasts.

In vivo

Doxycycline hyclate is an effective treatment for acute E. canis infection in dogs.

Doxycycline hyclate (5 mg/kg, orally) decreases the collagenase activity in corneas obtained from rabbits. Doxycycline hyclate (5 mg/kg, orally) promotes corneal reepithelialization in the rabbit alkali-burn model, a result, perhaps, of the drug's ability to inhibit excessive collagenase activity.

Doxycycline hyclate results in 43% of prophylaxis in orally treated mice, in contrast, the sustained-release doxycycline hyclate completely protects mice from infection and resultant pathology.

Doxycycline hyclate results in bioavailability of 70%, Cmin of 1 mg/L, Cmax of 2.3 mg/L and elimination half-life of 7 hours in calves with immature rumen function.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/15215128/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8498009/
  • [6] https://pubmed.ncbi.nlm.nih.gov/17166729/
  • [7] https://pubmed.ncbi.nlm.nih.gov/31204282/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot pATM / ATM HSP70 / HSP90 AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1
S4163-WB3
23282955
Immunofluorescence E-cadherin / Vimentin
S4163-IF1
29285218