NITD-349
Based on 1 publication(s) in Google Scholar
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.72%
- CAS 番号: 1473450-62-2
- 分子式: C17H20F2N2O
- 分子量:306.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 NITD-349
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生物活性
MIC50: 23 nM (Mycobacterium tuberculosis H37Rv)[1]
NITD-349 shows bactericidal activity against in vitro replicating Mycobacterium tuberculosis (Mtb) and also are active against intramacrophage Mtb. Kill kinetic analysis of these compounds showed both concentration- and time-dependent killing of Mtb cells with 3- to 4-log colony-forming unit (CFU) reductionwithin 3 days of treatment. The cidal activity profile of NITD-304 is similar to that of isoniazid for which rapid killing is noticed at concentrations greater than 0.2 μM. The MIC activity of NITD349 against various MDR Mtb strains ranges from 0.04 to 0.08 μM. NITD-349 shows high permeability and moderate in vitro metabolic clearance in mouse and human hepatic microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1473450-62-2
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性状 Solid
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分子量 306.35
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分子式 C17H20F2N2O
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Color White to off-white
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SMILES
O=C(C(N1)=CC2=C1C=C(F)C=C2F)NC3CCC(C)(C)CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Mol Biol
2020 Jul 24;432(16):4426-4434. PMID: 32512002
溶剤 & 溶解度
DMSO : ≥ 310 mg/mL (1011.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
For determining growth inhibition against nine diverse MDR Mtb clinical isolates, pellet formation method is used. MIC is defined as the minimum concentration of the drug required to inhibit 50% of H37Rv growth or 99% of growth in MDR clinical isolates after 5 or 10 days of incubation, respectively. Five milliliters of H37Rv culture (1 × 107 CFU/mL) is incubated with varying concentrations of NITD-349 for 6 days at 37°C, and an aliquot of culture is plated onto Middlebrook 7H11 agar plates; the CFU are enumerated after incubating plates for 3 weeks in a 37°C incubator[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mouse: In the acute murine efficacy model, mice are orally treated with a daily dose of NITD-349 (12.5, 25, 37.5, 50 mg/kg) for 4 weeks, 1 week after intranasal infection with low-dose Mtb (1000 CFU). Bacterial load in lungs (mean ± SD from six mice per group and per time point) is analyzed after treatment by enumerating CFU[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2642 mL | 16.3212 mL | 32.6424 mL | 81.6060 mL |
| 5 mM | 0.6528 mL | 3.2642 mL | 6.5285 mL | 16.3212 mL | |
| 10 mM | 0.3264 mL | 1.6321 mL | 3.2642 mL | 8.1606 mL | |
| 15 mM | 0.2176 mL | 1.0881 mL | 2.1762 mL | 5.4404 mL | |
| 20 mM | 0.1632 mL | 0.8161 mL | 1.6321 mL | 4.0803 mL | |
| 25 mM | 0.1306 mL | 0.6528 mL | 1.3057 mL | 3.2642 mL | |
| 30 mM | 0.1088 mL | 0.5440 mL | 1.0881 mL | 2.7202 mL | |
| 40 mM | 0.0816 mL | 0.4080 mL | 0.8161 mL | 2.0402 mL | |
| 50 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6321 mL | |
| 60 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3601 mL | |
| 80 mM | 0.0408 mL | 0.2040 mL | 0.4080 mL | 1.0201 mL | |
| 100 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8161 mL |