Zamicastat BIA 5-1058|cas:1080028-80-3|西域试剂

Zamicastat BIA 5-1058,98.0%

产品编号：Bellancom-106004| CAS NO：1080028-80-3| 分子式：C₂₁H₂₁F₂N₃OS| 分子量：401.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-106004	￥2500.00	杭州北京（现货）
Bellancom-106004	￥4500.00	杭州北京（现货）
Bellancom-106004	￥13500.00	杭州北京（现货）
Bellancom-106004	￥21000.00	杭州北京（现货）

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Zamicastat BIA 5-1058

产品介绍

Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂，可透过血脑屏障引起中枢和周边效应。Zamicastat 也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂，IC₅₀ 值分别为 73.8 μM 和 17.0 μM。Zamicastat 具有降血压作用。

生物活性

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC₅₀ values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.

体外研究

Following 4 hours of incubation (5, 10, 20, 50, 80, 100 μM), a significant loss of cell viability is verified with 100 μM Zamicastat (p=0.010) in MDCK-BCRP cells. No significant losses of cell viability are observed after 4 h of incubation for other concentrations in all cell lines. By decreasing the incubation period to 30 min, there is no significant loss of cell viability (p>0.05) at 100 μM in all cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	MDCK II, MDCK-MDR1 and MDCK-BCRP cells
Concentration:	5, 10, 20, 50, 80, 100 μΜ
Incubation Time:	4 hours (5, 10, 20, 50, 80, 100 μM) or 30 min (only 100 μM)
Result:	A significant loss of cell viability was verified with 100 μM in MDCK-BCRP cells.

体内研究
(In Vivo)

Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension in the Dahl SS rat. Zamicastat produces a dose-dependent decrease in blood pressure. 24 h after Zamicastat administration mean systolic blood pressure (SBP) decrease is -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively. Zamicastat administration also produces a significant 24-h average decrease in diastolic blood pressure (DBP) of - 14.6±3.4 mm Hg (P=0.0073) with 10 mg/kg body weight dose, -13.0±4.5 mm Hg (P=0.0347) with 30 mg/kg body weight dose and -15.0±3.1 mm Hg (P=0.0046) with 100 mg/kg body weight dose. Zamicastat administration leads to a decrease in the 24h post-dose mean arterial pressure (MAP) of -13.4±3.8 mm Hg (P=0.0162), -14.0±3.5 mm Hg (P=0.0101) and -20.6±3.7 mm Hg (P=0.0026) for the 10, 30, and 100 mg/kg body weight dose, respectively. There is a small, but significant, effect of Zamicastat on the 24-h mean heart rate (HR) post-dose for all tested doses (10 mg/kg: -19.1±3.2 beats/min, P=0.0019; 30 mg/kg: -13.0±4.5 beats/min, P=0.0347; 100 mg/kg: -21.6±6.6 beats/min, P=0.0235).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male inbred male Dahl SS rats
Dosage:	10, 30, or 100 mg/kg; 4 mL/kg
Administration:	Oral bolus, daily, seven days
Result:	Treatment produced a dose-dependent decrease in blood pressure. Twenty four hours after administration mean SBP decrease was -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively.

Animal Model:	ten-week-old male Wistar Han rats
Dosage:	30 mg/kg/day
Administration:	in animal feedings (mixed in meal rodent food) everyday
Result:	lead to a significant 51% decrease in noradrenaline levels excreted in urine

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male inbred male Dahl SS rats
Dosage:	10, 30, or 100 mg/kg; 4 mL/kg
Administration:	Oral bolus, daily, seven days
Result:	Treatment produced a dose-dependent decrease in blood pressure. Twenty four hours after administration mean SBP decrease was -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively.

Animal Model:	ten-week-old male Wistar Han rats
Dosage:	30 mg/kg/day
Administration:	in animal feedings (mixed in meal rodent food) everyday
Result:	lead to a significant 51% decrease in noradrenaline levels excreted in urine

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male inbred male Dahl SS rats
Dosage:	10, 30, or 100 mg/kg; 4 mL/kg
Administration:	Oral bolus, daily, seven days
Result:	Treatment produced a dose-dependent decrease in blood pressure. Twenty four hours after administration mean SBP decrease was -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively.

Animal Model:	ten-week-old male Wistar Han rats
Dosage:	30 mg/kg/day
Administration:	in animal feedings (mixed in meal rodent food) everyday
Result:	lead to a significant 51% decrease in noradrenaline levels excreted in urine

性状

Solid

溶解性数据

In Vitro:

DMSO : 150 mg/mL (373.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4908 mL	12.4542 mL	24.9085 mL
5 mM	0.4982 mL	2.4908 mL	4.9817 mL
10 mM	0.2491 mL	1.2454 mL	2.4908 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。