德拉马尼 T4202

Product Introduction
Bioactivity


英文名: Delamanid

描述: Delamanid (OPC-67683) 是一种新的分枝杆菌细胞壁合成抑制剂，可用于耐多药结核病。

激酶实验: In a 200 μL reaction volume, 1 μM TEM-1 is incubated with and without 5 μM Avibactam for 5 min at 37°C and subjected to two ultrafiltration cartridge (UFC) steps to remove excess inhibitor (Ultrafree-0.5 with Biomax membrane, 5-kDa cutoff). Centrifugation at 10,600× g for 8 min is performed at 4°C. After each ultrafiltration step, 20 μL retentate is diluted with 180 μL assay buffer to restore the original enzyme concentration. After two UFC treatments, the amount of free Avibactam is quantified by LC/MS/MS and found to be <5% of the original concentration. Loss of protein during UFC is assessed by measuring TEM-1 activity (on 4,000-fold dilution) in the acyl-enzyme sample compare with a non-UFC-treated enzyme, and loss is found to be <5%[1].

体外活性: In vitro: inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.[1] In in-vitro studies, delamanid shows more potent antibacterial activity against drug-susceptible and drug-resistant strains of M. tuberculosis.[2] Delamanid do not affect rifampin, pyrazinamide, and isoniazid exposure; the ethambutol AUCτ and Cmax values are about 25% higher with delamanid coadministration.

体内活性: In vivo: Twice-daily oral dosing of delamanid at 30 mg kg-1 for 5 days resulted in sterile cures in a mouse model of VL. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (93.55 mM)


关键字: Bacterial | inhibit | Inhibitor | OPC67683 | Antibiotic | Delamanid | OPC 67683

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途