Probenecid

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Probenecid

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

57-66-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
1g	询价
5g	询价

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	285.36
Cas No.	57-66-9
Formula	C₁₃H₁₉NO₄S
Solubility	insoluble in H2O; ≥13.66 mg/mL in EtOH; ≥8.7 mg/mL in DMSO
Chemical Name	4-(dipropylsulfamoyl)benzoic acid
Canonical SMILES	CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(=O)O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Probenecid是有机阴离子运输和多药耐药相关蛋白(MRP)的抑制剂[1，2]。Probenecid也可抑制pannexin-1通道，IC50值150 μM[3]。

MRPs是转运不同的分子穿过细胞膜的ATP结合带(ABC)转运者，并具有耐多药性。

Probenecid是有机阴离子运输、MRP和pannexin-1渠道的抑制剂。在MRP-过表达的HL60/AR和H69/AR肿瘤细胞系中，Probenecid以浓度依赖的方法逆转对道诺霉素(DNR）和长春新碱(VCR)的抗性[1]。在野生型AML-2细胞中，Probenecid以剂量和时间依赖的方式增加了MRP水平。在MRP-过表达的AML细胞中，Probenecid表现出显著的化学敏感效应。这些结果表明，Probenecid是一个有效的肿瘤细胞多药耐性(MDR)的化学敏感剂，也是MRP的激活剂[2]。

在缺血/再灌注(I/R)损伤大鼠中，Probenecid可防止CA1神经细胞死亡。Probenecid加强HSP70的上调，抑制Calpain-1的表达和组织蛋白酶B的释放。Probenecid也可抑制星形胶质细胞和小胶质细胞的增殖[4]。

参考文献：
[1]. Gollapudi S, Kim CH, Tran BN, et al. Probenecid reverses multidrug resistance in multidrug resistance-associated protein-overexpressing HL60/AR and H69/AR cells but not in P-glycoprotein-overexpressing HL60/Tax and P388/ADR cells. Cancer Chemother Pharmacol, 1997, 40(2): 150-158.
[2]. Kim HS, Min YD, Choi CH. Double-edged sword of chemosensitizer: increase of multidrug resistance protein (MRP) in leukemic cells by an MRP inhibitor probenecid. Biochem Biophys Res Commun, 2001, 283(1): 64-71.
[3]. Silverman W, Locovei S, Dahl G. Probenecid, a gout remedy, inhibits pannexin 1 channels. Am J Physiol Cell Physiol, 2008, 295(3): C761-767.
[4]. Wei R, Wang J, Xu Y, et al. Probenecid protects against cerebral ischemia/reperfusion injury by inhibiting lysosomal and inflammatory damage in rats. Neuroscience, 2015, 301: 168-177.

试验操作

Cell experiment:[1]
Cell lines	Wild-type and multidrug resistance protein (MRP)-overexpressing acute myelogenous leukemia (AML) cells, namely AML-2/WT and AML-2/DX100
Reaction Conditions	100, 200, 400 and 600 μM probenecid for 6 ~ 48 h incubation
Applications	Probenecid increased the MRP levels without an increase in MRP mRNA in AML-2/WT in both a time- and dose-dependent manner. Probenecid showed a marked chemosensitizing effect in AML-2/DX100.
Animal experiment:[2]
Animal models	Male Sprague-Dawley rats subjected to 20-min global cerebral ischemia/reperfusion (I/R) injury
Dosage form	0.1, 1 or 10 mg/kg (intravenously); 2 mg/kg (intraperitoneally); 5 mg/kg (orally) Administered intravenously, intraperitoneally, or by gavage before or after reperfusion
Applications	Probenecid via all three routes protected against CA1 neuronal death when given before reperfusion. This protective effect continued when probenecid was given at 2 h after reperfusion, but not at 6 h. Interestingly, the protective effect regained if probenecid was given continuously for 7 days after reperfusion. Probenecid protected against transient global cerebral I/R injury by inhibiting calpain-cathepsin pathway and the inflammatory reaction.
Note	The technical data provided above is for reference only.
	References: 1. Kim HS, Min YD, Choi CH. Double-edged sword of chemosensitizer: increase of multidrug resistance protein (MRP) in leukemic cells by an MRP inhibitor probenecid. Biochemical and Biophysical Research Communications, 2001, 283(1): 64-71. 2. Wei R, Wang J, Xu Y, et al. Probenecid protects against cerebral ischemia/reperfusion injury by inhibiting lysosomal and inflammatory damage in rats. Neuroscience, 2015, 301: 168-177.