Telacebec Q203; IAP6|cas:1334719-95-7|西域试剂

Telacebec Q203; IAP6,99.45%

产品编号：Bellancom-101040| CAS NO：1334719-95-7| 分子式：C₂₉H₂₈ClF₃N₄O₂| 分子量：557.01

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货号	价格	库存与货期
Bellancom-101040	￥650.00	杭州北京（现货）
Bellancom-101040	￥1800.00	杭州北京（现货）
Bellancom-101040	￥2800.00	杭州北京（现货）
Bellancom-101040	￥8250.00	杭州北京（现货）
Bellancom-101040	￥12400.00	杭州北京（现货）

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Telacebec Q203; IAP6

产品介绍

Telacebec (Q203) 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

Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against Mycobacterium tuberculosis H37Rv with an MIC₅₀ of 2.7 nM in culture broth medium.

体外研究

Imidazopyridine amide (IPA) compounds block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. The optimized IPA compound Telacebec (Q203) inhibits the growth of MDR and XDR Mycobacterium tuberculosis clinical isolates in culture broth medium in the low nanomolar range. Telacebec 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.

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

体内研究

Telacebec (Q203) is efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight. Telacebec displays pharmacokinetic and safety profiles compatible with once-daily dosing. Telacebec 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 Telacebec at 0.4, 2 and 10 mg per kg body weight, respectively.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (35.91 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (3.59 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.59 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明