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  2. Bacterial
  3. NITD-349

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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NITD-349

NITD-349 構造式

CAS 番号 : 1473450-62-2

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $135 在庫あり
25 mg $240 在庫あり
50 mg $360 在庫あり
100 mg $540 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

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製品説明

NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.

IC50 & Target

MIC50: 23 nM (Mycobacterium tuberculosis H37Rv)[1]

体外実験

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.

体内実験

In the acute murine efficacy modelNITD-349 shows favorable oral pharmacokinetic (PK) properties in rodents and dogs and are efficacious in mouse models of both acute and chronic Mycobacterium tuberculosis infection. In the acute murine efficacy model, treatment of mice with NITD-349 at doses of 12.5 and 50 mg/kg resulted in 0.9- and 3.4-log CFU reduction in lung tissue. In an established infection mouse model, after 2 weeks of treatment, the efficacy of NITD-349 is comparable to the first-line TB drug rifampicin and is better than ethambutol. Four weeks of treatment at 100 mg/kg with NITD-349 results in 2.38-log CFU reductions[1].

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

分子量

306.35

分子式

C17H20F2N2O

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N1)=CC2=C1C=C(F)C=C2F)NC3CCC(C)(C)CC3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2642 mL 16.3212 mL 32.6424 mL
5 mM 0.6528 mL 3.2642 mL 6.5285 mL
10 mM 0.3264 mL 1.6321 mL 3.2642 mL
View the 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.

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純度とドキュメンテーション
参考文献
細胞実験
[1]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

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
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
NITD-349
製品番号:
HY-109588
数量:
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