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IMT1B

CAS No. : 2304621-06-3

MCE 站：IMT1B

产品活性：IMT1B (LDC203974) 是一种具有口服活性的，非竞争性的，特异性的线粒体 RNA 聚合酶 (POLRMT) 别构抑制剂，可抑制线粒体 DNA (mtDNA) 的表达。IMT1B 具有抗肿瘤作用。

研究领域：Others

作用靶点：Others

In Vitro: IMT1B is a noncompetitive inhibitor that causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro.
IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells.
IMT1B depletes cellular metabolites.
IMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK.

In Vivo: IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts.
IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours.
IMT1B exhibits good oral bioavailability (mice 101 %) and C_max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg).
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).

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