| Identification | Back Directory | [Name]
TAM-16 | [CAS]
2030241-59-7 | [Synonyms]
TAM-16
5-Hydroxy-2-(4-hydroxyphenyl)-N-methyl-4-(piperidin-1-ylmethyl)benzofuran-3-carboxamide
3-Benzofurancarboxamide, 5-hydroxy-2-(4-hydroxyphenyl)-N-methyl-4-(1-piperidinylmethyl)- | [Molecular Formula]
C22H24N2O4 | [MOL File]
2030241-59-7.mol | [Molecular Weight]
380.44 |
| Chemical Properties | Back Directory | [Boiling point ]
609.9±55.0 °C(Predicted) | [density ]
1.288±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
8.97±0.15(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC50 value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel[1][2]. | [Biological Activity]
TAM16 is a potent and selective inhibitor of the thioesterase activity of Mycobacterium tuberculosis polyketide synthase Pks13. TAM16 is a highly potent bactericidal agent th at exhibits activity against drug-susceptible and drug-resistant clinical isolates of M. tuberculosis. It is effective in both acute and chronic mouse TB models. | [in vivo]
TAM-16 (compound 1; 200 mg/kg; p.o.; daily, for 14 days) prevents the development of characteristic lung lesions in murine TB infection models[2]. | Animal Model: | BALB/c mice with tuberculosis (TB) model[2] | | Dosage: | 200 mg/kg | | Administration: | oral administration; daily, for 14 days | | Result: | Had a significant reduction in lung CFU counts by ～0.9 log10 compared with the untreated control mice |
| [References]
[1] Scullion P, et, al. Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target. J Med Chem. 2022 Jan 13;65(1):409-423. DOI:10.1021/acs.jmedchem.1c01586
[2] Aggarwal A, et, al. Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13. Cell. 2017 Jul 13;170(2):249-259.e25. DOI:10.1016/j.cell.2017.06.025 |
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| Company Name: |
Shureli Biopharma Co.,Ltd
|
| Tel: |
0871-68355600 18787766125 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList1143315/0_EN.htm |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|