雷西那德|T6875

Lesinurad
878672-00-5

￥313 5mg 起订

￥452 10mg 起订

￥715 25mg 起订

上海更新日期：2025-03-12

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 雷西那德

英文名称：: Lesinurad

CAS号：: 878672-00-5

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：: 99.83%

产品类别：: 抑制剂

货号：: T6875

Product Introduction

Bioactivity

名称	Lesinurad
描述	Lesinurad (RDEA594) is a selective inhibitor of uric acid reabsorption which is used in combination with other agents in the therapy of gout. Lesinurad has had a limited clinical use but has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.
细胞实验	Lesinurad is solubilized in DMSO and stored, and then diluted with appropriate media before use[1]. Validated oocytes, HEK293, MDCK-II, Caco-2 or MDCK-MDR1 cell systems are used to study the interaction of Lesinurad with membrane transporters localized to the kidney (OAT1, OAT3, OCT2, MATE1, and MATE2K) or liver (P-gp, BCRP, OATP1B1, OATP1B3, and OCT1). Xenopus laevis oocytes are injected with OAT1 or OAT3 cRNA or control (water) while HEK293 cells are stably transfected with MATE1, MATE2K, or vector and MDCK-II cells with hOATP1B1, hOATP1B3, hOCT1, hOCT2, or vector. The MDCKII cell line is stably transfected with the human MDR1 gene to create a P-gp cell line. The interaction of Lesinurad with BCRP relied on the endogenous expression in Caco-2 cells. All cells are cultured with growth medium according to standard methodology. In order to determine whether Lesinurad is a substrate for a transporter, cells are incubated with [14C]-labeled Lesinurad at various concentrations and the amount of Lesinurad taken up by the cells determined by subtracting the uptake in vector cells from that in the transfected cells. The uptake of a [3H]-labeled known substrate of the transporter served as the positive control. Inhibition of a transporter by Lesinurad is determined by incubating cells with a fixed concentration of [3H]-labeled known substrate and various concentrations of unlabeled Lesinurad. Inhibition by a known inhibitor of each transporter served as the positive control. Cells are incubated for the appropriate amount of time. All reactions are terminated by the addition of ice-cold medium. The cells are then rinsed with medium and lysed[1].
体外活性	Lesinurad 以20倍于大鼠URAT1（rURAT1）的高效力抑制人体URAT1（hURAT1）的尿酸运输活动，其IC50分别为3.36和74.84 μM。Lesinurad通过涉及关键残基Phe365[1]的相互作用来抑制hURAT1。
体内活性	Lesinurad (RDEA594) 相比于其前体药物RDEA806展现了更佳的药动学特性。Lesinurad的100 mg剂量所展现的药理作用，相当于300 mg至800 mg RDEA806单剂量所产生的效果[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 : 50 mg/mL (123.68 mM) Ethanol : 50 mg/mL (123.7 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	SLC22A12 \| Inhibitor \| inhibit \| Lesinurad \| URAT1 \| Urate transporter 1 \| RDEA 594 \| RDEA-594
相关产品	Benzarone \| Puliginurad \| Dotinurad \| URAT1 inhibitor 7 \| 5-Fluoromethylornithine dihydrochloride \| Verinurad \| URAT1 inhibitor 1 \| Epaminurad HCl \| Indican \| Lingdolinurad \| Fraxin
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌上市药物库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA 上市药物库 \| 离子通道库 \| 膜蛋白靶向化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库

雷西那德|||来司诺雷|||RDEA594|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子