Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids^[1].

Delamanid inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex^[1].
Delamanid shows more potent antibacterial activity against drug-susceptible and drug-resistant strains of M. tuberculosis^[2].
Delamanid do not affect rifampin, pyrazinamide, and isoniazid exposure; the ethambutol AUCτ and Cmax values are about 25% higher with delamanid coadministration^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Delamanid (orally administration; 30 mg/kg; 5 days) results in sterile cures in a mouse model of VL^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

534.48

C₂₅H₂₅F₃N₄O₆

681492-22-8

迪拉马尼；地依麦迪；德拉马尼

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL (93.55 mM)

Ethanol : 2 mg/mL (3.74 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

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。

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    40% PEG300    5% Tween-80    45% saline

  Solubility: 2.5 mg/mL (4.68 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (4.68 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 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Sotgiu G et al. Delamanid (OPC-67683) for treatment of multi-drug-resistant tuberculosis. Expert Rev Anti Infect Ther. 2015 Mar;13(3):305-15.

  [2]. Xavier AS et al. Delamanid: A new armor in combating drug-resistant tuberculosis. J Pharmacol Pharmacother. 2014 Jul;5(3):222-4

  [3]. Mallikaarjun S et al. Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5976-85.

  [4]. Patterson S et al.The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis. Elife. 2016 May 24;5.