目錄:MedChemExpress LLC>>信號通路>> Remodelin hydrobromide | MedChemExpress
| CAS | 1622921-15-6 | 純度 | 99.49% |
|---|---|---|---|
| 分子量 | 363.28 | 分子式 | C??H??BrN?S |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號 | HY-16706A | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥/生物制藥 |
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CAS No. : 1622921-15-6
MCE 國際站：Remodelin hydrobromide
產(chǎn)品活性：Remodelin hydrobromide 是一種具有口服活性的乙?；D(zhuǎn)移酶 NAT10 的選擇性抑制劑。Remodelin hydrobromide 抑制前列腺癌細胞中 NAT10 活性，減緩 DNA 復(fù)制，抑制細胞生長。Remodelin hydrobromide 在異種移植模型中抑制前列腺癌和肝細胞性肝癌的生長，并能延長早年衰老綜合癥鼠模型的健康壽命。
研究領(lǐng)域：Epigenetics
作用靶點：Histone Acetyltransferase
In Vitro: Remodelin hydrobromide (10-40 μΜ, 1-7 days) inhibits NAT10 activity and cell proliferation with a dose-dependent manner in both AR-positive and AR-negative prostate cancer cells.
Remodelin hydrobromide (20 μΜ, 24 hours) inhibits NAT10 and slows DNA replication in prostate cancer cells.
Remodelin hydrobromide (1 μΜ, 7 days) decreases nuclear shape defects and increase genomic stability in LmnaG609G/G609G fibroblasts.
In Vivo: Remodelin hydrobromide (2 or 20 mg/kg, i.p., once every two days for 4 weeks) significantly reduces AR-negative prostate cancer tumor growth in tumor xenograft nude mice model.
Remodelin hydrobromide (100 mg/kg, p.o.) inhibits NAT10 and significantly enhances the healthspan in aLmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin hydrobromide (5 mg/kg, p.o.) shows a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice.
Pharmacokinetic parameters for Remodelin hydrobromide in Mice
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng/h/mL) | AUC0-? (ng/h/mL) | MRT_last (h) | F(%) |
| p.o. | 5 | 1.81 | 0.25 | 409 | 235 | 259 | 0.84 | 43.5% |
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