化合物Q203 T5400

Product Introduction
Bioactivity


英文名: Q203

描述: Q203 (Telacebec)是一种中氮杂吡啶酰胺。 在培养基中抑制结核分枝杆菌H37Rv 活性的MIC50值为2.7 nM。

体外活性: Q203 was active against the reference strain M. tuberculosis H37Rv at a minimum concentration required to inhibit the growth of 50% of organisms (MIC50) of 2.7 nM in culture broth medium and at an MIC50 of 0.28 nM inside macrophages [1]. Verapamil increased the potency of Q203 against Mycobacterium tuberculosis both in vitro and ex vivo [2]. Inhibition of cytochrome bd, a parallel branch of the mycobacterial respiratory chain, by aurachin D invoked bactericidal activity of Q203. Inhibition of respiratory chain activity by Q203 was incomplete, but could be enhanced by inactivation of cytochrome bd, either by genetic knock-out or by inhibition with aurachin D [3].

体内活性: Q203的生物可利用度为90%，终末半衰期为23.4小时。分布体积适中（5.27L/kg），系统清除率低（每分钟4.03ml/kg）。以10mg/kg的剂量，其促使细菌载量减少超过90%，这一效果与bedaquiline或isoniazid [1] 相当。

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

溶解度: DMSO : 18 mg/mL (32.3 mM)
H2O : Insoluble


关键字: Q203 | Q-203 | Antibiotic | IAP-6 | inhibit | Bacterial | IAP 6 | Q 203 | Inhibitor

相关产品: Colistin sulfate | (Z)-Ligustilide | LpxH-IN-AZ1 | Girinimbine | Dimethyl sulfoxide | Rhodojaponin V | (E)-Methyl 4-coumarate | Skullcapflavone II | Cefotiam Hexetil Hydrochloride | β-Lactamase-IN-2

相关库: Drug Repurposing Compound Library | Antibiotics Library | ReFRAME Related Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Bacterial Compound Library | Anti-Viral Compound Library | Anti-Infection Compound Library | Bioactive Compound Library

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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