阿曲生坦
基本信息
产品名称：
阿曲生坦
英文名称：
Atrasentan
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
522
更新日期：
2025-05-27
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: Atrasentan
描述: Atrasentan (ABT-627) 是内皮素受体 (endothelin receptor) 拮抗剂，能够抑制 ETA 的活性(IC50:0.0551 nM)。
细胞实验: All three prostate cancer cell lines (LNCaP, C4-2b, and PC-3 cells) are seeded at a density of 3 × 10^3 cells per well in 96-well microtiter culture plates. After overnight incubation, the medium is removed and replaced with a fresh medium containing different concentrations of ABT-627 (0-50 μM) diluted from a 10-mM stock. After 72 h of incubation with the drug, 20 μL of MTT solution (5 mg/mL in PBS) is added to each well and incubated further for 2 h. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in isopropanol (100 μL). The plates are mixed for 30 min on a gyratory shaker, and the absorbance is measured at 595 nm on a plate reader [2].
激酶实验: Cells are incubated and treated with Atrasentan. They are then washed twice with PBS and lysed in ice-cold lysis buffer [20 mM Tris (pH 7.4), 150 mM NaCl, 1% Triton X-100, 1 mM EDTA, 1 mM EGTA, 2.5 mM sodium PPi, 1 mM β-glycerophosphate, 1 mM sodium orthovanadate, 1 μg/mL leupeptin, and 1 mM PMSF]. The extracts are centrifuged to remove cellular debris, and the protein content of the supernatants is determined using the bicinchoninic acid (BCA) protein assay reagent. Proteins (150 μg) are incubated with gentle rocking at 4°C overnight with immobilized Akt antibody cross-linked to agarose hydrazide beads. After the Akt is selectively immunoprecipitated from the cell lysates, the immunoprecipitated products are washed twice with lysis buffer and twice with kinase assay buffer [25 mM Tris (pH 7.5), 10 mM MgCl2, 5 mM β-glycerol phosphate, 0.1 mM sodium orthovanadate, 2 mM DTT] and then resuspended in 40 μL of kinase assay buffer containing 200 μM ATP and 1 μg GSK-3α/β fusion protein. The kinase assay reaction is allowed to proceed at 30°C for 30 min and stopped by the addition of Lamelli SDS sample buffer. Reaction products are resolved by 10% SDS-PAGE, followed by Western blotting with antiphosphorylated GSK-3α/β antibody. For analysis of the total amount of Akt, 40 μg of protein from the lysate samples are resolved by 10% SDS-PAGE, followed by Western blotting with anti-Akt antibody [2].
动物实验: YM598 (0.3, 1, and 3 mg/kg), atrasentan (0.3, 1, and 3 mg/kg), or 0.5% methylcellulose as vehicle is orally administered to rats with a dosing cannula. The dosing volume of the test substances and vehicle is set at 5 mL/kg. Approximately 20 min after administration of compounds, the rats are anesthetized with sodium pentobarbital, and then pithed and ventilated 30 min after dosing. Approximately 1 h after oral administration of compounds, big endothelin-1 (1 nmol/kg) is intravenously administered, and blood pressure is measured. In these two experiments, the dose of test compound that causes 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis [1].
体外活性: Atrasentan (0-50 μM) 显著抑制LNCaP和C4-2b前列腺癌细胞生长。ABT-627与Taxotere联用，相较于单一药物处理，可引起更多活跃前列腺癌细胞的显著减少，并且在下调NF-κB DNA结合活性方面表现出更大程度的作用[2]。Atrasentan显著诱导多种CYPs及药物转运体的表达。它是一种中等程度的P-gp抑制剂（IC50：15.1 μM，于P388/dx细胞中）及一个弱BCRP抑制剂（IC50：59.8 μM，于MDCKII-BCRP细胞中）[3]。
体内活性: Atrasentan（3 mg/kg，p.o.）能够抑制大型内皮素-1（1 nmol/kg）在去髓大鼠中引起的血管加压反应[1]。在SCID-hu模型中，Atrasentan（10 mg/kg，i.p.）在一定程度上抑制了骨环境中C4-2b肿瘤的生长[2]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 9 mg/mL (17.63 mM)
关键字: A127722 | Endothelin Receptor | ABT627 | A 147627 | Inhibitor | inhibit | ABT 627 | A147627 | A 127722 | Atrasentan | A-127722
相关产品: Macitentan | Sulfisoxazole | BQ-123 | Edonentan | Ambrisentan | Sparsentan | Aminaftone | IRL 2500 | IRL-1038 acetate | RO 46-8443
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Diabetic Compound Library | Anti-Cancer Active Compound Library | Anti-Cardiovascular Disease Compound Library
Bioactivity
英文名: Atrasentan
描述: Atrasentan (ABT-627) 是内皮素受体 (endothelin receptor) 拮抗剂，能够抑制 ETA 的活性(IC50:0.0551 nM)。
细胞实验: All three prostate cancer cell lines (LNCaP, C4-2b, and PC-3 cells) are seeded at a density of 3 × 10^3 cells per well in 96-well microtiter culture plates. After overnight incubation, the medium is removed and replaced with a fresh medium containing different concentrations of ABT-627 (0-50 μM) diluted from a 10-mM stock. After 72 h of incubation with the drug, 20 μL of MTT solution (5 mg/mL in PBS) is added to each well and incubated further for 2 h. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in isopropanol (100 μL). The plates are mixed for 30 min on a gyratory shaker, and the absorbance is measured at 595 nm on a plate reader [2].
激酶实验: Cells are incubated and treated with Atrasentan. They are then washed twice with PBS and lysed in ice-cold lysis buffer [20 mM Tris (pH 7.4), 150 mM NaCl, 1% Triton X-100, 1 mM EDTA, 1 mM EGTA, 2.5 mM sodium PPi, 1 mM β-glycerophosphate, 1 mM sodium orthovanadate, 1 μg/mL leupeptin, and 1 mM PMSF]. The extracts are centrifuged to remove cellular debris, and the protein content of the supernatants is determined using the bicinchoninic acid (BCA) protein assay reagent. Proteins (150 μg) are incubated with gentle rocking at 4°C overnight with immobilized Akt antibody cross-linked to agarose hydrazide beads. After the Akt is selectively immunoprecipitated from the cell lysates, the immunoprecipitated products are washed twice with lysis buffer and twice with kinase assay buffer [25 mM Tris (pH 7.5), 10 mM MgCl2, 5 mM β-glycerol phosphate, 0.1 mM sodium orthovanadate, 2 mM DTT] and then resuspended in 40 μL of kinase assay buffer containing 200 μM ATP and 1 μg GSK-3α/β fusion protein. The kinase assay reaction is allowed to proceed at 30°C for 30 min and stopped by the addition of Lamelli SDS sample buffer. Reaction products are resolved by 10% SDS-PAGE, followed by Western blotting with antiphosphorylated GSK-3α/β antibody. For analysis of the total amount of Akt, 40 μg of protein from the lysate samples are resolved by 10% SDS-PAGE, followed by Western blotting with anti-Akt antibody [2].
动物实验: YM598 (0.3, 1, and 3 mg/kg), atrasentan (0.3, 1, and 3 mg/kg), or 0.5% methylcellulose as vehicle is orally administered to rats with a dosing cannula. The dosing volume of the test substances and vehicle is set at 5 mL/kg. Approximately 20 min after administration of compounds, the rats are anesthetized with sodium pentobarbital, and then pithed and ventilated 30 min after dosing. Approximately 1 h after oral administration of compounds, big endothelin-1 (1 nmol/kg) is intravenously administered, and blood pressure is measured. In these two experiments, the dose of test compound that causes 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis [1].
体外活性: Atrasentan (0-50 μM) 显著抑制LNCaP和C4-2b前列腺癌细胞生长。ABT-627与Taxotere联用，相较于单一药物处理，可引起更多活跃前列腺癌细胞的显著减少，并且在下调NF-κB DNA结合活性方面表现出更大程度的作用[2]。Atrasentan显著诱导多种CYPs及药物转运体的表达。它是一种中等程度的P-gp抑制剂（IC50：15.1 μM，于P388/dx细胞中）及一个弱BCRP抑制剂（IC50：59.8 μM，于MDCKII-BCRP细胞中）[3]。
体内活性: Atrasentan（3 mg/kg，p.o.）能够抑制大型内皮素-1（1 nmol/kg）在去髓大鼠中引起的血管加压反应[1]。在SCID-hu模型中，Atrasentan（10 mg/kg，i.p.）在一定程度上抑制了骨环境中C4-2b肿瘤的生长[2]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 9 mg/mL (17.63 mM)
关键字: A127722 | Endothelin Receptor | ABT627 | A 147627 | Inhibitor | inhibit | ABT 627 | A147627 | A 127722 | Atrasentan | A-127722
相关产品: Macitentan | Sulfisoxazole | BQ-123 | Edonentan | Ambrisentan | Sparsentan | Aminaftone | IRL 2500 | IRL-1038 acetate | RO 46-8443
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Diabetic Compound Library | Anti-Cancer Active Compound Library | Anti-Cardiovascular Disease Compound Library
公司简介
TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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