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Réf. Catalogue: S1835
Structure chimique
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | PMID |
|---|---|---|---|---|---|---|
| HeLa 299 | Antichlamydial assay | 44 to 48 hrs | Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay, IC50=0.727μM. | 29232584 | ||
| THP1 | Function assay | 30 mins | Drug uptake in human THP1 cells at pH 6 to 7 after 30 mins | 19564365 | ||
| THP1 | Function assay | 24 hrs | Drug uptake in human THP1 cells after 24 hrs in presence of verapamil | 19564365 | ||
| THP1 | Function assay | 24 hrs | Drug uptake in human THP1 cells after 24 hrs in presence of gemfibrozil | 19564365 | ||
| Hep2 | Antichlamydial assay | 4 ug/ml | 8 hrs | Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 4 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay | 32227948 | |
| Vero E6 | Antiviral assay | 2 days | Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50=2.12μM. | ChEMBL | ||
| Vero E6 | Antiviral assay | 2 days | Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90=8.65μM. | ChEMBL | ||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 748.98 | Formule | C38H72N2O12 |
Stockage (À compter de la date de réception) | |
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| N° CAS | 83905-01-5 | Télécharger le SDF | Stockage des solutions mères |
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| Synonymes | XZ-450,CP-62993 | Smiles | CCC1C(C(C(N(CC(CC(C(C(C(C(C(=O)O1)C)OC2CC(C(C(O2)C)O)(C)OC)C)OC3C(C(CC(O3)C)N(C)C)O)(C)O)C)C)C)O)(C)O | ||
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In vitro |
DMSO
: 100 mg/mL
(133.51 mM)
Ethanol : 100 mg/mL Water : Insoluble |
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In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
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.)
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.
| Targets/IC50/Ki |
protein synthesis
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|---|---|
| In vitro |
Azithromycin reduces about 40% of IL-8 mRNA and protein expression in cystic fibrosis (CF) cells reaching the levels of non-CF cells. This compound results in 50% and 70% reduction of NF-kappaB and AP-1 DNA binding, respectively, leading to levels of non-CF cells. It significantly enhances the intensity of a co-stimulatory molecule, CD80, on DCs but not CD86 and CD40 in dendritic cells (DCs). This macrolide significantly increases the production of IL-10 and Clarithromycin (CAM) significantly inhibits the production of IL-6 by DCs. It increases IL-10 and CAM decreases IL-2 productions significantly, when naive T cells derived from spleen are co-cultured with DCs treated in advance with LPS and these macrolides. This agent selectively inhibits fluid-phase endocytosis of horseradish peroxidase and lucifer yellow in J774 mouse macrophages. It delays sequestration of receptor-bound transferrin and peroxidase-anti-peroxidase immune complexes into cell-surface endocytic pits and vesicles. This chemical down-regulates cell surface transferrin receptors, but not Fc gamma receptors, by causing a major delay in the accessibility of internalized transferrin receptors to the recycling route, without slowing down subsequent efflux, resulting in redistribution of the surface pool to an intracellular pool. It inserts into the DOPC lipid bilayer, so as to decrease its cohesion and to facilitate the merging of DPPC into the DOPC fluid matrix.
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Références |
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(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT05972772 | Not yet recruiting | Infectious Disease|Therapeutics |
Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit|Mahidol Oxford Tropical Medicine Research Unit |
March 20 2024 | Phase 2|Phase 3 |
| NCT05796362 | Not yet recruiting | Infectious Disease|Drug Effect|Clinical Infection |
Brigham and Women''s Hospital|Bill and Melinda Gates Foundation |
April 2023 | Phase 1 |