solo para uso en investigación
Cat. No.: S4163
| Dianas relacionadas | HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP |
|---|---|
| Otros Antineoplastic and Immunosuppressive Antibiotics Inhibidores | Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Hygromycin B |
| 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 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| 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 |
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| 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 | ||
|
In vitro |
DMSO
: 100 mg/mL
(194.95 mM)
Water : 100 mg/mL Ethanol : Insoluble |
|
In vivo |
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Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
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.)
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.
| 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 |
|
| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | pATM / ATM HSP70 / HSP90 AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1 |
|
23282955 |
| Immunofluorescence | E-cadherin / Vimentin |
|
29285218 |