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  • 盐酸阿曲生坦|TQ0270|TargetMol

盐酸阿曲生坦|TQ0270|TargetMol

Atrasentan hydrochloride
195733-43-8
￥333 1mg 起订
￥826 5mg 起订
￥1180 10mg 起订
上海 更新日期：2026-04-02

TargetMol中国（陶术生物）

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联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
盐酸阿曲生坦
英文名称：
Atrasentan hydrochloride
CAS号：
195733-43-8
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
纯度规格：
99.75%
产品类别：
抑制剂
货号：
TQ0270

Product Introduction

Bioactivity

名称Atrasentan hydrochloride
描述Atrasentan hydrochloride (ABT-627 hydrochloride) is an antagonist of the endothelin receptor(IC50 = 55.1 μM for ETA).
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联合使用，相比单独使用任一化合物，可显著降低前列腺癌活细胞的数量，并更大程度地下调NF-κB DNA结合活性[2]。Atrasentan显著诱导多种CYPs和药物转运体的表达。它是一种中等强度的P-gp抑制剂（IC50：15.1 μM，在P388/dx细胞中）和一种弱BCRP抑制剂（IC50：59.8 μM，在MDCKII-BCRP细胞中）[3]。
体内活性Atrasentan（3 mg/kg, p.o.）通过抑制大型内皮素-1（1 nmol/kg）诱导的加压反应，在去髓大鼠中显示出效果[1]。此外，Atrasentan（10 mg/kg, i.p.）在SCID-hu模型中对C4-2b肿瘤在骨环境中的生长有一定程度的抑制作用[2]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度H2O : 0.4 mg/mL (0.73 mM), when pH is adjusted to 4 with HCl. Sonication and heating to 60℃ are recommended.
DMSO : 30 mg/mL (54.84 mM), Sonication is recommended.
0.1 M HCl : < 1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.66 mM), Sonication is recommended.
关键字Inhibitor | inhibit | ET-A | EndothelinReceptor | Endothelin Receptor | Atrasentan hydrochloride | Atrasentan | ABT-627 Hydrochloride | ABT627 Hydrochloride | ABT-627 | ABT627 | ABT 627 Hydrochloride | ABT 627 | A-147627 Hydrochloride | A147627 Hydrochloride | A-147627 | A147627 | A-127722 Hydrochloride | A127722 Hydrochloride | A 147627 Hydrochloride | A 147627 | A 127722 Hydrochloride | (+)-A 127722
相关产品Clazosentan | BQ-788 | Aprocitentan | SB-209670 | Edonentan | Macitentan | Sulfisoxazole | BMS 182874 | BMS 182874 hydrochloride | Bosentan | Ambrisentan | Sitaxsentan sodium
相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | FDA上市及药典收录分子库 | 上市药物库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 口服活性化合物库 | 药物功能重定位化合物库 | 疼痛相关化合物库 | 抗癌临床化合物库 | 抗癌药物库
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盐酸阿曲生坦|||ABT-627 hydrochloride|||A-147627 hydrochloride|||(+)-A 127722 hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (13年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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