Q203
(Synonyms: IAP6; Telacebec) 目录号 : GC19303
Q203 (IAP6) 是一种咪唑并吡啶酰胺化合物。
Cas No.:1334719-95-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: Sprague Dawley rats are used for pharmacokinetic studies. Compounds (Q203) are given at a dose of 2 mg per kg body weight intravenously or 10 mg per kg body weight orally. The compounds (Q203) are formulated in 20% TPGS (d-α tocopheryl polyethylene glycol 1000 succinate) for repeated-dose studies and in 40% PEG400, pH4 for single-dose studies. Blood samples are taken through the caudal vena cava using 1-mL syringes before perfusion. Samples are collected from three mice or rats at 0.5, 1, 2, 6, 12, 24 and 48 h post-dose. Blood samples are centrifuged at 3,200g for 10 min at 4 °C. Following centrifugation, plasma is collected and frozen until further analysis. Compound concentrations are determined by LC-MS[1]. Mice: Efficacy of Q203 in a mouse model of established tuberculosis is studied. Bacterial loads are enumerated in the lung of infected mice after 14 d and 28 d of treatment. Q203 is used at 0.4, 2 and 10 mg per kg body weight. Bedaquiline and isoniazid (INH) are used as positive controls at 6.5 and 15 mg per kg body weight, respectively. Five mice per group and per time point are used[1]. |
References: [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. | |
Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium.
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[1].
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[1].
References:
[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.
| Cas No. | 1334719-95-7 | SDF | |
| 别名 | IAP6; Telacebec | ||
| Canonical SMILES | O=C(C1=C(CC)N=C2C=CC(Cl)=CN21)NCC3=CC=C(N4CCC(C5=CC=C(OC(F)(F)F)C=C5)CC4)C=C3 | ||
| 分子式 | C29H28ClF3N4O2 | 分子量 | 557.01 |
| 溶解度 | DMSO : 20 mg/mL (35.91 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7953 mL | 8.9765 mL | 17.953 mL |
| 5 mM | 0.3591 mL | 1.7953 mL | 3.5906 mL |
| 10 mM | 0.1795 mL | 0.8976 mL | 1.7953 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。