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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 139 | 现货 | |
5 mg | ¥ 328 | 现货 | |
10 mg | ¥ 546 | 现货 | |
25 mg | ¥ 953 | 现货 | |
50 mg | ¥ 1,380 | 现货 | |
100 mg | ¥ 2,090 | 现货 | |
500 mg | ¥ 4,970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 388 | 现货 |
产品描述 | Delamanid (OPC-67683) is an anti-tuberculosis agent derived from the nitro-dihydro-imidazooxazole class of compounds that inhibits mycolic acid synthesis of bacterial cell wall. |
体外活性 | In vitro:抑制结核分枝杆菌复合体细胞壁的关键成分——粘酸的合成。[1] 在体外研究中,delamanid 对药物敏感和药物耐药的结核分枝杆菌菌株显示出更强的抗菌活性。[2] Delamanid 不影响利福平、吡嗪酰胺和异烟肼的暴露水平;与delamanid 合用时,乙胺丁醇的AUCτ和Cmax值约高出25%。 |
体内活性 | In vivo:每日两次口服delamanid,剂量为30 mg kg^-1,连续5日,在VL的小鼠模型中实现了无菌治愈。[4] |
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]. |
别名 | 迪拉马尼, 德拉马尼, OPC-67683 |
分子量 | 534.48 |
分子式 | C25H25F3N4O6 |
CAS No. | 681492-22-8 |
Smiles | C[C@]1(COc2ccc(cc2)N2CCC(CC2)Oc2ccc(OC(F)(F)F)cc2)Cn2cc(nc2O1)[N+]([O-])=O |
密度 | 1.45 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (93.55 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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