Home Microbiology Antineoplastic and Immunosuppressive Antibiotics inhibitor Tigecycline

solo para uso en investigación

Tigecycline Antineoplastic and Immunosuppressive Antibiotics inhibitor

Cat. No.: S1403

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. This compound induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
Tigecycline Antineoplastic and Immunosuppressive Antibiotics inhibitor Chemical Structure

Estructura química

Peso molecular: 585.65

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.86%
99.86

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
THP-1 Antibacterial assay 24 hrs Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine 19188393
Haga clic para ver más datos experimentales de líneas celulares

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

Peso molecular 585.65 Fórmula

C29H39N5O8

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 220620-09-7 Descargar SDF Almacenamiento de soluciones madre

Sinónimos GAR-936, WAY-GAR-936, TBG-MINO Smiles CC(C)(C)NCC(=O)NC1=CC(=C2CC3CC4C(C(=O)C(=C(C4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (170.75 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)

In vitro

Tigecycline evades the Tet(A-E) efflux pumps, which account for most acquired resistance to tetracycline and minocycline in Enterobacteriaceae and Acinetobacter spp. This compound binds to bacterial ribosomes that have been modified by the Tet(M) protein, a mechanism that compromises all available tetracyclines, and which is frequent in Gram-positive cocci and Neisseria spp. It remains vulnerable to the chromosomally-encoded multidrug efflux pumps of Proteeae and Pseudomonas aeruginosa, and to Tet(X), a tetracycline-degrading mono-oxygenase found, albeit rarely, in Bacteroides spp. Its MICs for enterococci, staphylococci, and streptococci are mostly 0.06–0.25 mg/L, again with little or no skew to the distribution. This agent is prone to oxidation, and MIC values, particularly for the most susceptible isolates, may be raised if the drug is added to broth that has become oxygenated during storage, or if drug-containing media are stored before inoculation. It is a poor substrate for tetracycline-specific efflux pumps, and it still attaches to ribosomes that have been modified by the Tet(M) protein. This antibacterial has demonstrated activity against a wide variety of gram-positive and gram-negative pathogens, including multidrug-resistant strains. It is active against many gram-positive and -negative organisms, including methicillin-resistantStaphylococcus aureus, vancomycin-intermediate and -resistant enterococci, and extended-spectrum β-lactamase–producing Escherichia coli and Klebsiella pneumoniae. This compound exhibits antibacterial activity against a wide spectrum of aerobic and anaerobic bacteria. It is a broad-spectrum, protein-inhibiting, antibacterial agent possessing activity against strains resistant to other chemotherapeutic agents. This chemical demonstrates in vitro activities against the GISA and the methicillin-resistant and methicillin-susceptible staphylococcal strains tested (MICs at which 90% of isolates tested are inhibited [MIC90s], 0.5 to 1 μg/ml). It has MIC90s of 0.25 μg/ml for all of the S. pneumoniae strains and demonstrates similar activities against all of the S. pneumoniae strains tested.

In vivo

Tigecycline is bactericidal against methicillin-susceptible S. aureus (MSSA) in the rabbit osteomyelitis model and exhibits good, but not excellent, activity in Legionellapneumophila pneumonia in guinea pigs. This compound at 50 mg/kg twice daily was not toxic to mice. It is effective in inhibiting NSCLC growth in vivo through decreasing proliferation and increasing apoptosis of tumor cells.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/27009695/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot E-cadherin / Vimentin CDK2 / Cyclin E Cox-1 / Cox-2 / Cox-4 p-AMPKα / AMPKα / p-mTOR / mTOR / p-p70S6K / p70S6K / p-4E-BP-1 / 4E-BP1 p62 / LC3-I / LC3-II Cyclin D1 / CDK2 / p21
S1403-WB6
26621850
Growth inhibition assay Cell viability
S1403-viability1
30247801

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
NCT06049771 Recruiting
Carbapenem-resistant Enterobacteriaceae
Phramongkutklao College of Medicine and Hospital|Silpakorn University
 September 17 2023 Not Applicable
NCT05698160 Not yet recruiting
Blood Coagulation Disorder
The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
 May 1 2023 --
NCT04937894 Recruiting
Infectious Disease
Shandong University|Shandong Provincial Hospital
 June 1 2021 --
NCT04724798 Unknown status
Extracorporeal Membrane Oxygenation|Pharmacokinetics|Tigecycline
Nanfang Hospital Southern Medical University
 January 20 2020 --
NCT04489459 Unknown status
Treatment of Blood Stream Infections Due to Multidrug-Resistant Klebsiella Pneumoniae
Al-Azhar University
 September 21 2019 Phase 4