| Identification | Back Directory | [Name]
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- | [CAS]
2304621-06-3 | [Synonyms]
(S)-1-((R)-2-(4-(2-chloro-4-fluorophenyl)-2-oxo-2H-chromen-7-yloxy)propanoyl)piperidine-3-carboxylic acid
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- | [Molecular Formula]
C24H21ClFNO6 | [MDL Number]
MFCD33402174 | [MOL File]
2304621-06-3.mol | [Molecular Weight]
473.88 |
| Chemical Properties | Back Directory | [Boiling point ]
705.7±60.0 °C(Predicted) | [density ]
1.426±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.33±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects[1]. | [in vivo]
IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts[1].
IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours[1].
IMT1B exhibits good oral bioavailability (mice 101 %) and Cmax (mice 5149 ng/mL) following oral administration (mice 10 mg/kg)[1].
IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (mice 0.44 L/h/kg) following intravenous administration (mice 1 mg/kg)[1].
| Animal Model: | 7-9 weeks female BALB/c nude mice, with A2780 cells xenograft[1] | | Dosage: | 100 mg/kg | | Administration: | Oral administration, daily, for four weeks | | Result: | Led to a clear reduction of tumour volume. |
| Animal Model: | Mice[1] | | Dosage: | 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | Oral bioavailability (101%), Cmax (5149 ng/mL), T1/2 (1.88 h). |
| [References]
[1] Nina A Bonekamp, et al. Small-molecule inhibitors of human mitochondrial DNA transcription. Nature. 2020 Dec;588(7839):712-716. DOI:10.1038/s41586-020-03048-z |
|
|