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製品番号: HY-W064918

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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。

CAS 番号: 1473450-60-0
分子式: C₁₇H₂₀Cl₂N₂O
分子量:339.26

保管条件:

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

Data Sheet (272 KB)

NITD-304 構造式

CAS 番号: 1473450-60-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 1473450-60-0
分子量 339.26
分子式 C₁₇H₂₀Cl₂N₂O
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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