A-192621|cas:195529-54-5|西域试剂

A-192621,99.0%

产品编号：Bellancom-120295| CAS NO：195529-54-5| 分子式：C₃₃H₃₈N₂O₆| 分子量：558.66

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货号	价格	库存与货期
Bellancom-120295	￥2900.00	杭州北京（现货）
Bellancom-120295	￥4700.00	杭州北京（现货）
Bellancom-120295	￥9800.00	杭州北京（现货）

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A-192621

产品介绍

A-192621 是一种有效的非肽，口服活性，选择性内皮素 B (ET_B) 受体拮抗剂，IC₅₀ 为 4.5 nM，K_i 为 8.8 nM。A-192621 的选择性比 ET_A 高 636 倍 (IC₅₀ 为 4280 nM，K_i 为 5600 nM)。A-192621 促进 PASMC 细胞凋亡，并引起动脉血压升高和血浆 ET-1 水平升高。

生物活性

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ET_B) receptor antagonist with an IC₅₀ of 4.5 nM and a K_i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET_A (IC₅₀ of 4280 nM and K_i of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.

体外研究

A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner.
A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment.

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

Cell Viability Assay

Cell Line:	Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration:	1 μM, 10 μM, 50 μM, 100 μM
Incubation Time:	72 hours
Result:	The viability of PASMCs was significantly decreased in a dose-dependent manner.

Western Blot Analysis

Cell Line:	Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration:	1 μM, 10 μM, 100 μM
Incubation Time:	72 hours
Result:	The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.

体内研究
(In Vivo)

A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ET_B with an ED₅₀ value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ET_A. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat.

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

Animal Model:	Male Sprague-Dawley rats (250-350 g)
Dosage:	30 mg/kg 100 mg/kg
Administration:	Oral administration; daily; for 3 days
Result:	Inhibited both dilatory and pressor responses induced by S6c mediated by ET_B with an ED₅₀value of 30 mg/kg.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (250-350 g)
Dosage:	30 mg/kg 100 mg/kg
Administration:	Oral administration; daily; for 3 days
Result:	Inhibited both dilatory and pressor responses induced by S6c mediated by ET_B with an ED₅₀value of 30 mg/kg.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (250-350 g)
Dosage:	30 mg/kg 100 mg/kg
Administration:	Oral administration; daily; for 3 days
Result:	Inhibited both dilatory and pressor responses induced by S6c mediated by ET_B with an ED₅₀value of 30 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (179.00 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7900 mL	8.9500 mL	17.9000 mL
5 mM	0.3580 mL	1.7900 mL	3.5800 mL
10 mM	0.1790 mL	0.8950 mL	1.7900 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 (4.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.47 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