NITD-304
NITD-304 is an orally active anti-tuberculosis agent. NITD-304 exerts inhibitory and bactericidal activities gainst Mycobacterium tuberculosis and multidrug-resistant Mycobacterium tuberculosis. NITD-304 inhibits mycobacterial cell wall biosynthesis and demonstrates synergistic or additive growth inhibitory activity with select antibacterial agents. NITD-304 shows low risk of cardiotoxicity and drug-drug interactions, with no inhibition of major cytochrome P-450 enzymes or hERG channel. NITD-304 can be used for the research of tuberculosis and multidrug-resistant tuberculosis.
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- CAS No.: 1473450-60-0
- 화학식: C17H20Cl2N2O
- 분자량:339.26
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
10.5 μg/mL
Compound: NITD-304
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Cytotoxicity against African green monkey vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against African green monkey vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
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[PMID: 35915958] |
NITD-304 (5 days) potently inhibits growth of virulent Mtb H37Rv with an MIC50 of 0.015 μM after 5 days of incubation[1].
NITD-304 (10 days) inhibits 99% growth of diverse MDR Mtb clinical isolates at concentrations from <0.04 to 0.08 μM after 10 days of incubation[1].
NITD-304 (0.04-5.00 μM; 1-6 days) induces concentration- and time-dependent bactericidal activity against Mtb H37Rv[1].
NITD-304 (0.1-5 μM; 5 days) reduces intracellular Mtb burden in activated THP-1 macrophages in a concentration-dependent manner[1].
NITD-304 (0-100 μM) induces iniB reporter activity in M. bovis BCG, indicating it inhibits mycobacterial cell wall biosynthesis[1].
NITD-304 exhibits no significant in vitro cytotoxicity or genotoxicity, low risk of hERG-mediated cardiotoxicity, and no inhibition of major cytochrome P-450 enzymes[1].
NITD-304 (5 days) has reduced activity against Mtb with mmpL3 gene mutations, increasing its MIC50 to 0.052-0.222 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mycobacterium tuberculosis H37Rv
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Concentration:0.04, 0.2, 1, 5 μM
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Incubation Time:1, 3, 6 days
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Result:Induced concentration- and time-dependent bactericidal activity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (male/female unspecified; intranasally infected with Mycobacterium tuberculosis H37Rv, 1 week infection establishment before treatment)[1]
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Dosage:12.5 mg/kg; 25 mg/kg; 37.5 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:Achieved a 1.24-log CFU reduction in lung tissue compared to untreated controls.
Achieved a 3.82-log CFU reduction in lung tissue compared to untreated controls.
Reached a minimum effective dose (MED) of 37.5 mg/kg, with corresponding plasma Cmax of 2 μM and AUC of 19.5 μM/hour.
Achieved a 1.11-log CFU reduction in lung tissue compared to untreated controls after 2 weeks of treatment with 100 mg/kg.
Achieved a 2.14-log CFU reduction in lung tissue compared to untreated controls after 4 weeks of treatment with 100 mg/kg.
Chemical Information
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CAS No. 1473450-60-0
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분자량 339.26
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화학식 C17H20Cl2N2O
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SMILES
O=C(NC1CCC(C)(CC1)C)C2=CC3=C(C=C(C=C3Cl)Cl)N2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Rao SP, et al. Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis. Sci Transl Med. 2013;5(214):214ra168. [Content Brief]
[2]. Li W, et al. Synergistic Interactions of MmpL3 Inhibitors with Antitubercular Compounds In Vitro. Antimicrob Agents Chemother. 2017;61(4):e02399-16. Published 2017 Mar 24. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NITD-304 Related Classifications
Cat. No.: HY-W064918
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- NITD-304
- 1473450-60-0
- NITD304
- NITD 304
- Bacterial
- intramacrophage Mycobacterium tuberculosis
- multidrug-resistant Mycobacterium tuberculosis
- THP-1 macrophages
- hERG channel
- mycobacterial cell walls
- MmpL3
- cytochrome P-450 enzymes
- Mycobacterium tuberculosis
- trehalose monomycolate transport
- mycolic acid export
- Inhibitor
- inhibitor
- inhibit