化合物SQ109 T16925

Product Introduction
Bioactivity


英文名: SQ109

描述: SQ109 (NSC-722041) 是一种有效的锥鞭毛体形式的寄生虫抑制剂 (IC50 = 50 nM)。 SQ109 是一种抗结核药物，靶向 MmpL3。

体外活性: SQ109 causes major ultrastructural changes in all three life cycle forms. SQ109 inhibits extracellular epimastigotes (IC50 = 4.6μM) and the clinically relevant intracellular amastigotes (IC50 = 0.5 - 1 μM), with a selectivity index of 10 to 20. SQ109 has little effect (EC50 = 80 μM) in a red blood cell hemolysis assay[1].

体内活性: The t1/2 of SQ109 in dogs (12-29 h, mean 29.3 h) is longer than in rats (7-8 h, mean 7.4 h), as reflected by the significantly larger volume of distribution of SQ109 in dogs. The oral bioavailability of SQ109 in rats and dogs is 12% and 5%, respectively[2]. SQ109 (0.1-25 mg/kg) to the mice for 28 days results in dose-dependent reductions of mycobacterial load in both spleen and lung comparable to that of EMB(100 mg/kg), but is less potent than isoniazid(25 mg/kg). Pharmacokinetic profiles of SQ109 in mice following a single administration showed its Cmax as 1038 (i.v.) and 135 ng/mL (p.o.), with an oral Tmax of 0.31 h and an oral bioavailability of 4%. The elimination t1/2 of SQ109 is 3.5 (i.v.) and 5.2 h (p.o.)[3].

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

溶解度: DMSO : 25 mg/mL (75.63 mM)


关键字: Parasite | SQ 109 | NSC-722041 | NSC722041 | Bacterial | Inhibitor | SQ109 | inhibit | Antibiotic | SQ-109

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相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Parasitic Compound Library | Orally Active 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