Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 6,490 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,220 | 现货 |
产品描述 | Atrasentan (ABT-627) (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA). |
靶点活性 | ETA:0.055 nM |
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]。 |
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]. |
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]. |
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]. |
别名 | A-147627, (+)-A 127722, 阿曲生坦, ABT-627 |
分子量 | 510.62 |
分子式 | C29H38N2O6 |
CAS No. | 173937-91-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9 mg/mL (17.63 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9584 mL | 9.792 mL | 19.584 mL | 48.9601 mL |
5 mM | 0.3917 mL | 1.9584 mL | 3.9168 mL | 9.792 mL | |
10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.896 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Atrasentan 173937-91-2 GPCR/G Protein Endothelin Receptor A127722 ABT627 A 147627 A-147627 Inhibitor (+)-A 127722 阿曲生坦 ABT-627 inhibit ABT 627 A147627 A 127722 A-127722 inhibitor