NITD-349 |
Catalog No.GC32166
One-Click Copy Product Info
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NITD-349는 독성 결핵균 H37Rv에 대해 23nM의 MIC50으로 강력한 항마이코박테리아 활성을 나타내는 MmpL3 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1473450-62-2
Sample solution is provided at 25 µL, 10mM.
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NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
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].
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].
[1]. Rao SP, et al. Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis. Sci Transl Med. 2013 Dec 4;5(214):214ra168.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Rao SP, et al. Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis. Sci Transl Med. 2013 Dec 4;5(214):214ra168. | |
| Cas No. | 1473450-62-2 | SDF | |
| Canonical SMILES | O=C(C(N1)=CC2=C1C=C(F)C=C2F)NC3CCC(C)(C)CC3 | ||
| Formula | C17H20F2N2O | M.Wt | 306.35 |
| Solubility | DMSO : ≥ 310 mg/mL (1011.91 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2642 mL | 16.3212 mL | 32.6424 mL |
| 5 mM | 652.8 μL | 3.2642 mL | 6.5285 mL |
| 10 mM | 326.4 μL | 1.6321 mL | 3.2642 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)