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Macozinone (PBTZ169) 是具有杀菌作用的苯并噻嗪酮,也有抗结核作用。它也是一种 DprE1有效抑制剂,可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。
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Macozinone (PBTZ169) 是具有杀菌作用的苯并噻嗪酮,也有抗结核作用。它也是一种 DprE1有效抑制剂,可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 178 | 现货 | |
5 mg | ¥ 447 | 现货 | |
10 mg | ¥ 696 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,230 | 现货 | |
100 mg | ¥ 3,190 | 现货 | |
200 mg | ¥ 4,360 | 现货 |
产品描述 | Macozinone (PBTZ169) inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043. |
体外活性 | PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. |
体内活性 | PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). |
别名 | PBTZ169 |
分子量 | 456.48 |
分子式 | C20H23F3N4O3S |
CAS No. | 1377239-83-2 |
Smiles | [O-][N+](=O)c1cc(cc2c1sc(nc2=O)N1CCN(CC2CCCCC2)CC1)C(F)(F)F |
密度 | no data available |
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: 4.56 mg/mL (10 mM), Sonication is recommended. ![]() | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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