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SQ109
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SQ109图片
CAS NO:502487-67-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
NSC 722041
产品介绍
SQ109 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。

产品描述

SQ109 is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets 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].

Cas No.

502487-67-4

分子式

C22H38N2

分子量

330.55

别名

NSC 722041

储存和溶解度

DMSO:25 mg/mL (75.63 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years