Q203 (Synonyms: Q203; IAP6)
目录号: PL14707 纯度: ≥99%
CAS No. :1334719-95-7
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中文名称
Q203
中文别名
6-氯-2-乙基-N-[[4-[4-[4-(三氟甲氧基)苯基]-1-哌啶基]苯基]甲基]咪唑并[1,2-a]吡啶-3-甲酰胺;6-chloro-2-ethyl-N-[(4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}phenyl)methyl]imidazo[1,2-a]pyridine-3-carboxamide
英文名称
Q203
英文别名
Q203;IAP6;Q-203;55G92WGH3X;MMV687696;6-chloro-2-ethyl-n-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo[1,2-a]pyridine-3-carboxamide;Telacebec;6-chloro-2-ethyl-N-[(4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}phenyl)methyl]imidazo[1,2-a]pyridine-3-carboxamide;6-chloro-2-ethyl-N-[[4-[4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl]phenyl]methyl]imidazo[1,2-a]pyridine-3-carboxamide;Telacebec (USAN/INN);IAP6; Telacebec; Q203;BCP2;MTB H37Rv;MTB H37Ra
Cas No.
1334719-95-7
分子式
C29H28ClF3N4O2
分子量
557.01
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Q203(IAP6)是中氮杂吡啶酰胺化合物。 在培养基中抑制结核分枝杆菌H37Rv活性的MIC50值为2.7 nM。
生物活性
Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC 50 of 2.7 nM in culture broth medium.
性状
Solid
IC50 & Target[1][2]
MIC50: 2.7 nM (Mycobacterium tuberculosis H37Rv)
体外研究(In Vitro)
Imidazopyridine amide (IPA) compounds block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. The optimized IPA compound Q203 inhibits the growth of MDR and XDR Mycobacterium tuberculosis clinical isolates in culture broth medium in the low nanomolar range. Q203 is active against the reference strain Mycobacterium tuberculosis H37Rv with MIC50s of 2.7 nM in culture broth medium and 0.28 nM inside macrophages. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Q203 is efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight. Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Q203 has a bioavailability of 90% and a terminal half-life of 23.4 h. The volume of distribution is moderate (5.27 l per kg body weight), and the systemic clearance is low (4.03 mL/min per kg). After 4 weeks of treatment, reductions of 90%, 99% and 99.9% in M. tuberculosis H37Rv bacterial load is observed in the groups treated with Q203 at 0.4, 2 and 10 mg per kg body weight, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Pethe K, et al. Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. Nat Med. 2013 Sep;19(9):1157-60.
溶解度数据
In Vitro: DMSO : 20 mg/mL (35.91 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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