Delamanid
(Synonyms: 德拉马尼; OPC-67683) 目录号 : GC19122An antimycobacterial compound
Cas No.:681492-22-8
Sample solution is provided at 25 µL, 10mM.
Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.In vitro: inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.[1]In in-vitro studies, 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] In vivo: Twice-daily oral dosing of delamanid at 30 mg kg-1 for 5 days resulted in sterile cures in a mouse model of VL. [4]
References:
[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.
Cas No. | 681492-22-8 | SDF | |
别名 | 德拉马尼; OPC-67683 | ||
Canonical SMILES | FC(F)(F)OC1=CC=C(OC2CCN(C3=CC=C(OC[C@@]4(C)CN5C(O4)=NC([N+]([O-])=O)=C5)C=C3)CC2)C=C1 | ||
分子式 | C25H25F3N4O6 | 分子量 | 534.48 |
溶解度 | DMSO : ≥ 50 mg/mL (93.55 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.871 mL | 9.3549 mL | 18.7098 mL |
5 mM | 0.3742 mL | 1.871 mL | 3.742 mL |
10 mM | 0.1871 mL | 0.9355 mL | 1.871 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet