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- 文献和实验
- 技术资料
- CAS号：
878672-00-5
- 规格：
1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥287.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥266.0 |
| 规格： | 10mg | 产品价格： | ￥361.0 |
| 规格： | 25mg | 产品价格： | ￥572.0 |
| 规格： | 50mg | 产品价格： | ￥952.0 |
| 规格： | 100mg | 产品价格： | ￥1512.0 |
| 规格： | 200mg | 产品价格： | ￥2280.0 |
| 规格： | 500mg | 产品价格： | ￥3704.0 |
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/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (24.74 mM), Solution. 10% DMSO+90% Saline : < 10 mg/mL (24.74 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 250 mg/mL (618.38 mM), Sonication is recommended. Ethanol : 50 mg/mL (123.68 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | Urate transporter 1 | URAT1 | SLC22A12 | RDEA-594 | RDEA 594 | OAT3 | OAT1 | Lesinurad | Inhibitor | inhibit |
| 相关产品 | Benzarone | Hydrastine | Puliginurad | Dotinurad | Mulberrin | URAT1 inhibitor 7 | Cabotegravir sodium | Cabotegravir | Epaminurad HCl | Indican | Lingdolinurad | Fraxin |
| 相关库 | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library | Bioactive Compounds Library Max | EMA Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | FDA-Approved Drug Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Metabolism Disease Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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1.103.90±0.95(1.20-5.00)138±2.90134_2.60(128-145)5.25±0.135.40±0.15(4.85-5.85)108±0.60107±0.55(105-110)26.2±2.1024.8±2.30(20.2-31.5)5.60±1.616.55±1.30(2.30-9.20)5.60±0.407.40±0.50(3.20-8.50)3.11±0.371.38±0.28(0.80-3.90)大鼠0.35±0.020.24±0.07(0.00-0.55)28
时间安排，不过至少你自己暂时完成任务解放了 ～ 二、心态调整 & 目标拆解 不要觉得 1 天写完 Results 不可能，那是你没用对方法，心态没调整好。初稿而已，不是让你一口气写完直接投稿，初稿到投稿之间还有好几轮的修稿呢。 不要一口气想着完美，先想着完成，目标定的不一样，你的行动力大不相同。现在就问你，一天的时间，写完 Results，ok 不？ 具体做法： 要提前告知身边人，要闭关写作了，找一个不被打扰的空间，自己安排好学习时间。比如，9：00-11：00 是学习高效期，再提前半个小时做好准备，如打开
连接技术 M8、M12、开放式终端 SMT 电特性 短路保护 极性容错保护 过载保护 德国费斯托稀罕产品型号信息给大家公布让大家摆脱型号询价的问题： MFH-5/3G-1/4-B 19787 1151.00 LFR
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￥266 - 3704
