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Etamicastat hydrochloride (BIA 5-453 hydrochloride) 是一种外周选择性多巴胺β-羟化酶抑制剂,具有降低高血压的作用。
Etamicastat hydrochloride (BIA 5-453 hydrochloride) 是一种外周选择性多巴胺β-羟化酶抑制剂,具有降低高血压的作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,230 | 现货 | |
5 mg | ¥ 3,150 | 现货 | |
10 mg | ¥ 4,560 | 现货 | |
25 mg | ¥ 6,900 | 现货 | |
50 mg | ¥ 9,490 | 现货 | |
100 mg | ¥ 12,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,460 | 现货 |
产品描述 | Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension. |
靶点活性 | DBH:107 nM |
体外活性 | Etamicastat hydrochloride 抑制hERG电流幅度,IC50值为44 μg/mL[1]。 |
体内活性 | Etamicastat hydrochloride(50 mg/kg;单次口服)在雄性Wistar大鼠中表现出中等口服生物利用度(64%)、最大血药浓度(Cmax=4.9 nM)和终末消除半衰期(T1/2=3.7小时)。而Etamicastat hydrochloride (100 mg/kg;腹腔注射)显著降低了心脏的去甲肾上腺素水平并同时增加了多巴胺水平[1]。 |
细胞实验 | Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL . |
动物实验 | Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats.Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels. |
别名 | 依他米司特盐酸盐, BIA 5-453 hydrochloride |
分子量 | 347.81 |
分子式 | C14H16ClF2N3OS |
CAS No. | 677773-32-9 |
Smiles | Cl.NCCc1c[nH]c(=S)n1[C@H]1COc2c(F)cc(F)cc2C1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 15.0 mg/mL (43.1 mM), Sonication is recommended. DMSO: 90.0 mg/mL (258.8 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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