化合物 AZ876|T5178|TargetMol

AZ876
898800-26-5

￥397 1mg 起订

￥843 5mg 起订

￥1240 10mg 起订

上海更新日期：2024-12-12

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：: 化合物 AZ876

英文名称：: AZ876

CAS号：: 898800-26-5

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.

纯度规格：: 99.41%

产品类别：: 抑制剂

货号：: T5178

Product Introduction

Bioactivity

名称	AZ876
描述	AZ876 is a potent, highly selective LXR agonist with Ki/EC50 of 7/6 nM and 11/73 nM for hLXRα and hLXRβ respectively.
激酶实验	Binding vectors for His-tagged protein production were prepared by inserting the ligand-binding domain cDNA of human LXRα (amino acids 205–447) in pET28 and the ligand-binding domain cDNA of LXRβ (amino acids 216–461) in pET24D. Proteins were expressed in Escherichia coli and purified on Ni+ columns. Binding assays using LXRα and LXRβ protein were run by adding reagents to Wallac Isoplate 1450–514. Briefly, each 96 plate well contained assay buffer (20 mM Tris pH 7.5, 80 mM NaCl, 2 mM dithiothreitol, 0.125% Chaps and 10% glycerol), 0.1 mg SPA beads (polylysine-coated yttrium silicate beads), LXRα (0.5 μg) or LXRβ (0.25 μg), 30 nM 3H-ligand (specific activity of 473 Kbq/nmol) and test compound in a 10-point dose-response dilution. The assay mixture was shaken gently for 2 h on a plate shaker after which the beads were allowed to settle for 1 hour before counting. Transactivation vectors were prepared by inserting the ligand-binding domain cDNA sequences of human or mouse LXRα and LXRβ in frame with the yeast Gal4 transcription factor DNA binding domain and the nuclear localization signal from the T-antigen of polyomavirus in the eucaryotic expression vector pSG5. The ligand-binding domain cDNA of human LXRα and LXRβ was the same as mentioned previously. The mouse sequence corresponded to amino acids 203–445 for LXRα and amino acids 201–446 for LXRβ. The vectors were co-transfected with a pGL3 luciferase reporter plasmid containing a minimal SV40 promoter and five copies of the UAS Gal4 recognition site into U2/OS osteosarcoma cells. Ligands were added as 10-point dose-response curves and then luciferase activity was measured after 48 h [1].
动物实验	Cardiac hypertrophy was induced in male C57Bl6/J mice via transverse aortic constriction (TAC) for 6 weeks. During this period, sham and TAC-operated mice were randomized to receive either regular chow (control) or chow supplemented with AZ876 (20 μmol/kg/day). Cardiac function was assessed with echocardiography and invasive haemodynamics. In vitro studies were performed in isolated neonatal rat ventricular myocytes (NRVMs) and adult rat cardiac fibroblasts. Leucine and proline tracer assays were used to measure protein and collagen synthesis, respectively [2].
体外活性	AZ876抑制了与肥大和纤维化相关基因的上调，并进一步抑制了促肥大和促纤维化的TGFβ-Smad2/3信号通路。在心肌细胞中，AZ876处理后的细胞中，苯肾上腺素刺激的细胞肥大显著减少。在心脏成纤维细胞中，AZ876阻止了TGFβ和血管紧张素II诱导的成纤维细胞胶原合成，并抑制了肌成纤维细胞标志物α-平滑肌肌动蛋白[2]的上调。
体内活性	低剂量AZ876在血浆或肝脂肪上无影响，相比之下，高剂量AZ876升高了血浆中的甘油三酯并降低了胆固醇水平。低剂量AZ876减少了病变面积；而高剂量AZ876显著减少了病变面积、病变数量及严重性。AZ876的任何剂量都不影响病变组成[1]。在C57Bl6/J小鼠中，通过横向主动脉缩窄（TAC）引发心脏肥大，持续6周。在此期间，小鼠饲料中添加或不添加AZ876（20μmol/kg/天）。在小鼠心脏中，LXRα蛋白表达量因TAC反应上调约7倍。LXR激活剂AZ876缓和了这一增加，并显著减少了由TAC引起的心脏重量增加、心肌纤维化和心脏功能障碍，同时不影响血压[2]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (125.12 mM) 5% DMSO+40% PEG300+5% Tween 80+50% Saline : 2.5 mg/mL (5.69 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字	AZ-876 \| Liver X receptor \| LXR \| AZ 876 \| Inhibitor \| AZ876 \| inhibit
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AZ876|TargetMol

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	(12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
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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