1. Anti-infection
  2. Bacterial
  3. 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.

For research use only. We do not sell to patients.

NITD-304

NITD-304 Chemical Structure

CAS No. : 1473450-60-0

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Description

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[1][2].

Cellular Effect
Cell Line Type Value Description References
Vero IC50
10.5 μg/mL
Compound: NITD-304
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
[PMID: 35915958]
In Vitro

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.

Cell Viability Assay[1]

Cell Line: Mycobacterium tuberculosis H37Rv
Concentration: 0.04, 0.2, 1, 5 μM
Incubation Time: 1, 3, 6 days
Result: Induced concentration- and time-dependent bactericidal activity.
In Vivo

NITD-304 (12.5-100 mg/kg; p.o.; daily; 4 weeks) dose-dependently reduces Mycobacterium tuberculosis lung burden in an acute mouse tuberculosis model, with a minimum effective dose of 37.5 mg/kg[1].

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

Animal Model: BALB/c mice (male/female unspecified; intranasally infected with Mycobacterium tuberculosis H37Rv, 1 week infection establishment before treatment)[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 37.5 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 4 weeks
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.
Molecular Weight

339.26

Formula

C17H20Cl2N2O

CAS No.
SMILES

O=C(NC1CCC(C)(CC1)C)C2=CC3=C(C=C(C=C3Cl)Cl)N2

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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HY-W064918
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