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4°C, sealed storage, away from moisture
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
1622921-15-6
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥660.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥600.0 |
| 规格： | 10 mg | 产品价格： | ￥790.0 |
| 规格： | 25 mg | 产品价格： | ￥1800.0 |
| 规格： | 50 mg | 产品价格： | ￥2900.0 |
| 规格： | 100 mg | 产品价格： | ￥4000.0 |
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Remodelin hydrobromide
CAS No. : 1622921-15-6
MCE 国际站：Remodelin hydrobromide
产品活性：Remodelin hydrobromide 是一种具有口服活性的乙酰基转移酶 NAT10 的选择性抑制剂。Remodelin hydrobromide 抑制前列腺癌细胞中 NAT10 活性，减缓 DNA 复制，抑制细胞生长。Remodelin hydrobromide 在异种移植模型中抑制前列腺癌和肝细胞性肝癌的生长，并能延长早年衰老综合症鼠模型的健康寿命。
研究领域：Epigenetics
作用靶点：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
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| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng/h/mL) | AUC0-Ꝏ (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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