Aprocitentan-ACT-132577-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAprocitentanCat. No.: HY-15895CAS No.: 1103522-45-7Synonyms: ACT-132577分式: CHBrNOS分量: 546.19作靶点: Endothelin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 46 mg/

2、mL (84.22 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8309 mL 9.1543 mL 18.3086 mL5 mM 0.3662 mL 1.8309 mL 3.6617 mL10 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Aprocitentan (ACT-132577)是maci

3、tentan 的主要活性代谢物，为 ETA/ETB 双重 抑制剂。体外研究 Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 onnonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell lineA10 and mouse fibroblast cell line 3T3) 1.1/2 Master of

4、 Small Molecules 您边的抑制剂师www.MedChemE体内研究 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 Aproc

5、itentan (ACT-132577) in rat plasma ranges from 101.4%to 115.2% 2.户使本产品发表的科研献 BMC Cancer. 2018 Feb 6;18(1):154.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Iglarz M, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Ph

6、armacol Exp Ther.2008 Dec;327(3):736-45.2. Zhang J, et al. Pharmacokinetic study of ACT-132577 in rat plasma by ultra performance liquid chromatography-tandem massspectrometry. Int J Clin Exp Med. 2015 Oct 15;8(10):18420-6McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-82