Q203 纯度:98.01% 50mg

您好！欢迎来到炼石商城请登录注册兼职小伙伴

我的购物车

Qiagen 凯杰 Biosharp Omega

客服热线 0771-3293894

首页酶、辅酶及抑制剂MCE>

图片仅供参考，请以实物为准

Q203 纯度:98.01% 50mg

市场价：: 0.00

促销价：: ¥0.00

货号：HY-101040

品牌：MCE

配送至：

北京朝阳

支付：账期货到付款

数量：

支 (预计4-5工作日到货(以MCE官网货期为准))

亲，想了解价格请QQ咨询客服！

工作时间

周一至周五：9:00-18:00

咨询电话

0771-3293894

在线咨询

: 客服郭恒蔡玉坤曾宪飞技术咨询

浏览了该商品的用户最终购买

RNeasy Mini Kit (50) 50次

3720.00

Plasmid Mini Kit I(200) 200...

576.00

10ul吸头，透明，袋装，可灭菌...

85.80

浏览了该商品的用户还浏览了

QIAfilter Plasmid Maxi Kit (...

3000.00

QIAamp DNA Blood Midi Kit (2...

2680.00

QIAamp UCP Pathogen Mini Kit...

4112.00

商品介绍
商品咨询

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。

Description

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.

IC₅₀ & Target

MIC50: 2.7 nM (Mycobacterium tuberculosis H37Rv)^[1]

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^[1].

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^[1].

Clinical Trial

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7953 mL	8.9765 mL	17.9530 mL
5 mM	0.3591 mL	1.7953 mL	3.5906 mL
10 mM	0.1795 mL	0.8976 mL	1.7953 mL

* Please refer to the solubility information to select the appropriate solvent.

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.

Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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.

Animal Administration
^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References