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NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $44 | In Stock | |
25 mg | $80 | In Stock | |
50 mg | $133 | In Stock | |
100 mg | $200 | In Stock | |
200 mg | $283 | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
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 |
Smiles | CC1(C)CCC(CC1)NC(=O)c1cc2c(F)cc(F)cc2[nH]1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 310 mg/mL (1011.91 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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