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NITD-916

Name: NITD-916
Brand: TargetMol
SKU: T60774
Price: 328 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: NITD916, NITD 916) Copy Product Info

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Synonyms: NITD916, NITD 916

Catalog No. T60774 Copy Product Info

Purity: 99.78%

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NITD-916, a 4-hydroxy-2-pyridone derivative, is a mycobacterial enoyl reductase InhA inhibitor (IC50=570 nM) with oral activity and high lipophilicity. Capable of forming a ternary complex with InhA and NADH, blocking fatty acyl substrate binding and inhibiting mycolic acid synthesis, thereby exerting potent anti-tuberculosis effects.

Cas No. 1614262-83-7

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Pack Size	Price	USA Stock	Global Stock
1 mg	$328	In Stock	In Stock
5 mg	$798	In Stock	In Stock
10 mg	$1,090	-	In Stock
25 mg	$1,590	-	In Stock
1 mL x 10 mM (in DMSO)	$547	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.78%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

NITD-916 AI Summary

NITD-916 exhibits significant antimycobacterial activity against Mycobacterium tuberculosis, with MIC50 values ranging from 30.0 nM to 80.0 nM in glycerol-containing medium. It effectively inhibits Mycobacterium tuberculosis ATCC 25618 InhA enzyme, with an IC50 of 570.0 nM when using trans-2-dodecenoyl-CoA as a substrate. Additionally, it demonstrates notable cytotoxicity against human liver cancer cells and strong inhibitory effects on drug-resistant strains of Mycobacterium tuberculosis, leading to significant reductions in bacterial counts in both lung and spleen tissues. NITD-916 also possesses favorable pharmacokinetic properties, including good oral bioavailability in mice, high solubility, and rapid clearance in both human and mouse liver microsomes..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	NITD-916, a 4-hydroxy-2-pyridone derivative, is a mycobacterial enoyl reductase InhA inhibitor (IC50=570 nM) with oral activity and high lipophilicity. Capable of forming a ternary complex with InhA and NADH, blocking fatty acyl substrate binding and inhibiting mycolic acid synthesis, thereby exerting potent anti-tuberculosis effects.
Targets & IC50	InhA:570 nM
In vitro	Methods: The broth microdilution method was used to detect the in vitro activity of NITD-916, with Mycobacterium abscessus standard strains and clinical isolates as test organisms, incubated in CaMHB medium at 30°C for 3–5 days, at concentrations of 1.25×, 10×, and 20× MIC; meanwhile, intracellular bactericidal experiments were performed using THP-1 macrophages with an MOI of 2:1, incubated for 1–3 days. Results: NITD-916 showed low MIC against both smooth and rough type strains, and 10× MIC significantly reduced intracellular bacterial load. [1] Methods: The nutrient starvation model was used to detect the in vitro activity of NITD-916, with Mycobacterium tuberculosis H37Rv as the test organism. Non-replicating bacteria were prepared by starvation culture in PBS for 2 weeks, then NITD-916 (0.14–0.58 μM) was added with a final DMSO concentration of 2%, and continuously incubated for 21 days. CFU was determined by plate counting method. Results: NITD-916 showed time-dependent bactericidal activity, reducing viable bacterial counts by more than 3 log units within 21 days, with no drug-resistant mutant strains growing. [2]
In vivo	Methods: An acute pulmonary infection mouse model was used, in which 6-week-old male BALB/c mice were infected intranasally with Mycobacterium abscessus and treated with NITD-916 (100 mg/kg) dissolved in microemulsion preconcentrate by daily oral gavage for 14 consecutive days; control groups received rifabutin, clarithromycin, or blank vehicle. Results: NITD-916 reduced pulmonary bacterial load by 5.6 log₁₀ CFU in mice, with significant improvement in lung lesions and inflammation, showing superior efficacy to clarithromycin and comparable efficacy to rifabutin. [3] Methods: A Mycobacterium tuberculosis-infected mouse model was used to validate the in vivo activity of NITD-916. Drug was administered via oral route in both acute and chronic infection models, with dose and treatment duration following conventional anti-tuberculosis regimens, and vehicle meeting preclinical dosing standards. Results: NITD-916 demonstrated in vivo efficacy comparable to isoniazid, effectively reducing pulmonary bacterial load, with significantly lower resistance incidence than isoniazid, and showed good safety and tolerability. [4]
Synonyms	NITD916, NITD 916

Chemical Properties

Molecular Weight	311.42
Formula	C₂₀H₂₅NO₂
Cas No.	1614262-83-7
Smiles	OC1=C(C2=CC=CC=C2)C(=O)NC(CC3CCC(C)(C)CC3)=C1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 15 mg/mL (48.17 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2111 mL	16.0555 mL	32.1110 mL	160.5549 mL
5 mM	0.6422 mL	3.2111 mL	6.4222 mL	32.1110 mL
10 mM	0.3211 mL	1.6055 mL	3.2111 mL	16.0555 mL
20 mM	0.1606 mL	0.8028 mL	1.6055 mL	8.0277 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.