sALT629
sALT629 is an orally active antitubercular agent with potent intramacrophage activity (EC50 = 1.5 μM). sALT629 shows broad-spectrum anti-Mycobacterium tuberculosis (Mtb) activities across four carbon sources, equipotent efficacy against drug-resistant Mtb, and activity against both slow-replicating and nonreplicating Mtb. sALT629 exhibits synergistic activity when combined with oxazolidinone drugs, such as Linezolid (HY-10394) and Sutezolid (HY-10392). sALT629 can be used for the research of tuberculosis.
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- No. CAS: 484026-63-3
- Fòrmula: C13H17N5O2
- Peso molecular:275.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
sALT629 (0.96-12.5 μM) exhibits inhibitory activity against Mtb cultured on four carbon sources (acetate, butyrate, cholesterol, glucose), with an EC50 of 1.5 μM against intramacrophage Mtb, an MIC of 0.8-1.7 μM against multidrug-resistant (MDR), extensively drug-resistant (XDR), and single-drug-resistant Mtb strains, and activity against slow-replicating and nonreplicating Mtb[1].
sALT629 (1.7-13.6 μM; 7 days) shows dose-dependent bactericidal activity against Mtb in 7H12 cholesterol media[1].
sALT629 (20 μM; 7 days) reduces CFU by approximately 1.5-log in the Hu-Coates 100-day dormancy model and by 0.5-log in Loebel's nutritionally deprived model[1].
sALT629 (>40 μM) shows no significant cytotoxicity against HEK293T and HepG2 cells, with a SI greater than 23[1].
sALT629 exhibits synergistic activity when combined with oxazolidinone drugs (Linezolid (HY-10394), Sutezolid (HY-10392)) with an FIC of 0.5, additive effects with drugs such as TBD11, TBA-7371 (HY-19750), and Q203 (HY-101040) (FIC=0.63-1.0), and no significant interaction with Isoniazid (HY-B0329) and other agents (FIC>1.0)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | MRT0-last | AUC0-last | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 20 mg/kg | p.o. | 文献审核 | 5,610 ng/mL | 0.83 h | 2.96 h | 2.85 h | 17,551 ng·h/mL | 55.1 % |
sALT629 (100 mg/kg BID, or 200 mg/kg QD, p.o., for 4 consecutive days) shows plasma concentrations remaining above EC50 for over 24 hours, and lung tissue exposure exceeds EC50[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 484026-63-3
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Peso molecular 275.31
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Fòrmula C13H17N5O2
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SMILES
O=C(CN1N=NC(C2=CC=C(C=C2)OCC(C)C)=N1)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
sALT629 Related Classifications
HY-179649 Related Classifications
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