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NITD-349

Catalog No. T12231   CAS 1473450-62-2

NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.

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NITD-349 Chemical Structure
NITD-349, CAS 1473450-62-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 222.00
50 mg In stock $ 372.00
100 mg In stock $ 556.00
500 mg In stock $ 1,220.00
1 mL * 10 mM (in DMSO) In stock $ 79.00
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Purity: 99.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
Targets&IC50 Mycobacterium tuberculosisH37Rv:23 nM (MIC50)
In vitro NITD-304 and NITD-349, showed potent activity against both drug-sensitive and multidrug-resistant clinical isolates of Mtb. Promising pharmacokinetic profiles of both compounds after oral dosing in several species enabled further evaluation for efficacy and safety. NITD-304 and NITD-349 were efficacious in treating both acute and chronic Mtb infections in mouse efficacy models. Furthermore, dosing of NITD-304 and NITD-349 for 2 weeks in exploratory rat toxicology studies revealed a promising safety margin. Finally, neither compound inhibited the activity of major cytochrome P-450 enzymes or the hERG (human ether-a-go-go related gene) channel[1].
In vivo 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].
Molecular Weight 306.35
Formula C17H20F2N2O
CAS No. 1473450-62-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 310 mg/mL (1011.91 mM)

TargetMolReferences and Literature

1. Rao SP, et al. Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis. Sci Transl Med. 2013 Dec 4;5(214):214ra168. 2. Yang X , Hu T , Yang X , et al. Structural Basis for the Inhibition of Mycobacterial MmpL3 by NITD-349 and SPIRO[J]. Journal of Molecular Biology, 2020, 432(16).

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Anti-Infection Compound Library Bioactive Compounds Library Max Anti-Bacterial Compound Library

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Keywords

NITD-349 1473450-62-2 Microbiology/Virology Others Antibacterial inhibit Bacterial NITD349 NITD 349 Inhibitor inhibitor

 

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