Aprocitentan

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Aprocitentan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1103522-45-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议

产品名称

ACT-132577

产品介绍

Aprocitentan (ACT-132577) 是 Macitentan 的主要活性代谢物。Aprocitentan 是双重ETA/ETB拮抗剂，IC₅₀分别为 3.4 nM 和 987 nM，pA₂值分别为 6.7 和 5.5。

生物活性

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dualETA/ETBantagonist withIC₅₀s of 3.4 nM and 987 nM, andpA₂valus of 6.7 and 5.5, respectively^[1].

IC₅₀& Target^[1]

ET_A

3.4 nM (IC₅₀)

ET_A

6.7 (pA2)

ET_B

987 nM (IC₅₀)

ET_B

5.5 (pA2)

体外研究
(In Vitro)

Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3)^[1].

体内研究
(In Vivo)

Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat^[1]. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%^[2].

Clinical Trial

分子量

546.19

性状

Solid

Formula

C₁₆H₁₄Br₂N₆O₄S

CAS 号

1103522-45-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 46 mg/mL(84.22 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	1.8309 mL	9.1543 mL	18.3086 mL
5 mM	0.3662 mL	1.8309 mL	3.6617 mL
10 mM	0.1831 mL	0.9154 mL	1.8309 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。