solo per uso di ricerca
N. Cat.: S4163
Struttura chimica
| Target correlati | HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP |
|---|---|
| Altro Antineoplastic and Immunosuppressive Antibiotics Inibitori | 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 |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | 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 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 512.94 | Formula | C22H24N2O8.1/2C2H6O.HCl.1/2H2O |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 24390-14-5 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | 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 |
|||||
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
| 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. |
Riferimenti |
|
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | pATM / ATM HSP70 / HSP90 AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1 |
|
23282955 |
| Immunofluorescence | E-cadherin / Vimentin |
|
29285218 |
(dati da https://clinicaltrials.gov, aggiornato il 2026-05-15)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT06738407 | RECRUITING | Gonorrhea; Chlamydia; Syphilis; Sexually Transmitted Infections (STIs) |
Westat |
2026-02-27 | PHASE4 |
| NCT07688096 | NOT_YET_RECRUITING | Ehlers-Danlos Syndrome Hypermobility Type (hEDS); Ehlers-Danlos Syndrome (EDS); Joint Hypermobility; Joint Instability; Hypermobility Spectrum Disorder; Chronic Pain Syndrome; Musculoskeletal Pain; Sprain; Subluxation; Dislocation; Craniocervical Disfunction |
Manhattan Pain Medicine, PLLC |
2026-07-15 | PHASE1; PHASE2 |
| NCT04504123 | RECRUITING | Exudative Macular Degeneration; Wet Age-related Macular Degeneration |
University of Iowa |
2020-11-04 | PHASE2 |
| NCT04762134 | RECRUITING | Bacterial Sexually Transmitted Diseases |
Jonathan Troy Grennan |
2023-06-02 | |
| NCT04582383 | ACTIVE_NOT_RECRUITING | Acne |
University of Pennsylvania |
2022-03-30 | PHASE4 |
| NCT05112211 | RECRUITING | Thyroid Associated Ophthalmopathy |
Sun Yat-sen University |
2022-01-01 |