IMT1B
规格
| Cas Number | 2304621-06-3(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | DNA/RNA Synthesis,Cell Cycle/DNA Damage,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | IMT1B (LDC203974) 是线粒体 RNA 聚合酶 (POLRMT) 的一种口服活性、非竞争性和特异性异构体抑制剂，可抑制线粒体 DNA (mtDNA) 的表达。IMT1B 具有抗肿瘤作用。 |
| 英文描述 |
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 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. ?\nIMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells. ?\nIMT1B depletes cellular metabolites. ?\nIMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A2780 cells Concentration: 0.01 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM Incubation Time: 72 hours, 96 hours, 168 hours Result: Decreased cell viability in a dose-dependent manner. In Vivo IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts . ?\nIMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours . ?\nIMT1B exhibits good oral bioavailability (mice 101 %) and C max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg) . ?\nIMT1B 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 7-9 weeks female BALB/c nude mice, with A2780 cells xenograft Dosage: 100 mg/kg Administration: Oral administration, daily, for four weeks Result: Led to a clear reduction of tumour volume. Animal Model: Mice Dosage: 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (101%), C max (5149 ng/mL), T 1/2 (1.88 h). IC50& Target:POLRMT |