| 货号 | 14981-5g |
| 描述 | Probenecid is a benzoic acid derivative that inhibits organic anion transporters (OATs) but activates the transient receptor potential (TRP) channel TRPV2. It inhibits OAT1, OAT3, and OAT6 with Ki values of 6.3, 9.0, and 8.4 µM, respectively, as well as OAT2 with an IC50 value of 0.67 µM.1,2,3 It is a poor inhibitor of the organic cation transporters OCT1 and OCT2 (IC50 = 1.6 and 1.7 mM, respectively).4 Through its effects on OATs, probenecid enhances the renal excretion of urate, alleviating gout, while reducing the elimination of many medications.5 It also acts as an agonist of TRPV2 (EC50 = 31.9 µM), eliciting nociceptive behavior under inflammatory conditions in mice.5 |
| 别名 | Benemid;NSC 18786;Tubophan;Uricosid; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kaler, G.,Truong, D.M.,Khandelwal, A., et al. Structural variation governs substrate specificity for organic anion transporter (OAT) homologs. Potential remote sensing by OAT family members. The Journal of Biological Chemisty 282(33), 23841-23853 (2007). 2.Takeda, M.,Narikawa, S.,Hosoyamada, M., et al. Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. European Journal of Pharmacology 419(2-3), 113-120 (2001). 3.Khamdang, S.,Takeda, M.,Shimoda, M., et al. Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. Journal of Pharmacological Sciences 94(2), 197-202 (2004). 4.Arndt, P.,Volk, C.,Gorboulev, V., et al. Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. American Journal of Physiology.Renal Physiology 281(3), F454-F468 (2001). 5.Robbins, N.,Koch, S.E.,Tranter, M., et al. The history and future of probenecid. Cardiovasc.Toxicol. 12(1), 1-9 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 285.4 |
| 分子式 | C13H19NO4S |
| CAS号 | 57-66-9 |
| 稳定性 | ≥ 2 years |
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