Probenecid - Moligand™, 10mM in DMSO , Solute carrier family 22 member 11 inhibitor, CAS No.57-66-9, Solute carrier family 22 member 11 inhibitor

CAS: 57-66-9 Cat. No.: P408015 Peso molecular: 285.36 Número EC: 200-344-3

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-(Di-n-propylaminosulfonyl)benzoic acid | 4-(Di-n-propylsulfamoyl)benzoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Probenecid Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport , which is also a TRPV2 agonist and an inhibitor of TAS2R16 . Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker.
In vitro

Probenecid is able to prevent the efflux of calcium-sensitive fluorescent dyes during studies of cellular calcium mobilization. Probenecid (2.5 mM) is found to block the export of Fura-2 from 1321N1 astrocytoma cells, and does not change the basal calcium concentration or the muscarinic calcium response. Probenecid is a potent transient receptor potential vanilloid 2 (TRPV2) agonist. Probenecid selectively induces increase in intracellular Ca²⁺ influx in HEK293T cells transiently expressing exogenous TRPV2. Probenecid is able to interact with organic anion transporters (OAT). 0.1 mM Probenecid efficiently inhibits ATP-dependent active vesicular N-ethylmaleimide glutathione (NEM-GS) uptake by Human Multidrug Resistance Proteins 1 (MRP1) and MRP2. In isolated Sf9 cell membranes, Probenecid stimulates ATPase activity of MRP2 with approximate KACT of 250 μM, but inhibits ATPase activity of MRP1. Probenecid is an inhibitor of the hTAS2R16, hTAS2R38, and hTAS2R43 bitter taste receptors. 1 mM Probenecid attenuates saccharin-induced calcium flux responses of hTAS2R16 to near baseline levels. Probenecid dose-dependently inhibits hTAS2R16 (in the presence of 3 mM salicin) and hTAS2R38 (in the presence of 300 μM PTC). This activity is independent of Probenecid\'s activity as a transport inhibitor, but is concerning with Probenecid interaction with the receptor.

In vivo

Probenecid is an inhibitor of organic transport in vivo. Probenecid is able to decrease the renal clearance of antibiotic, such as penicillin, which enhances serum levels of antibiotic. Probenecid enhances the renal excretion of urate by acting as a competitive inhibitor of OAT, which prevents OAT-mediated reuptake of uric acid from the urine to the serum. Probenecid is found to block acid metabolites from exiting the central nervous system, and is a competitive inhibitor of monoamine transport in the kidney, liver, and the eye.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

4-(Di-n-propylaminosulfonyl)benzoic acid | 4-(Di-n-propylsulfamoyl)benzoic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ACTIVATOR, ANTAGONIST, INHIBITOR

Mecanismo de acción

Solute carrier family 22 member 11 inhibitor

Propiedades del producto

• ALogP: 3.2

Nombres e identificadores

• Isómeros SMILES: CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(=O)O
• WGK Alemania: 3
• RTECS: DG9400000
• Número ONU: 3249
• Grupo de embalaje: II
• Peso molecular: 285.36
• Reaxy-Rn: 2815775
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2815775&ln=

Objetivos asociados (humanos)

SLC22A6 Tclin Solute carrier family 22 member 6 (1 Activities)

Discover Target: SLC22A6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRPV2 Tchem Transient receptor potential cation channel subfamily V member 2 (1 Activities)

Discover Target: TRPV2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA2 Tclin Carbonic anhydrase 2 (3 Activities)

Discover Target: CA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CA9 Tclin Carbonic anhydrase 9 (3 Activities)

Discover Target: CA9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 198-199°C

Referencias

1. Xiao Fei, Jiang Haizhou, Li Zi, Jiang Xiaoxue, Chen Shanghai, Niu Yuguo, Yin Hanrui, Shu Yousheng, Peng Bo, Lu Wei, Li Xiaoying, Li Zhigang, Lan Shujue, Xu Xiaoyan, Guo Feifan.  (2023)  Reduced hepatic bradykinin degradation accounts for cold-induced BAT thermogenesis and WAT browning in male mice.  Nature Communications,  14  (1): (1-17).  [PMID:37130842] [10.1038/s41467-023-38141-0]

2. Fan Wu, Ting Zhao, Yu Zhang, Yan Wang, Guoxin Liao, Baojing Zhang, Chao Wang, Xiangge Tian, Lei Feng, Bangjiang Fang, Xiaokui Huo, Xiaochi Ma.  (2023)  Beneficial herb-drug interaction of rhein in Jinhongtang and Imipenem/Cilastatin mediated by organic anion transporters.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:37023835] [10.1016/j.jep.2023.116449]

3. Chen Sun, Mingyu Zhang, Yanhong Zhao, Jianxin Pang, Ying Peng, Jiang Zheng.  (2020)  An LC-MS/MS- and hURAT1 cell-based approach for screening of uricosuric agents.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:32905987] [10.1016/j.jchromb.2020.122336]

4. Qingquan Zeng, Mengru Bai, Cui Li, Shuanghui Lu, Zhiyuan Ma, Yunchun Zhao, Hui Zhou, Huidi Jiang, Dongli Sun, Caihong Zheng.  (2019)  Multiple Drug Transporters Contribute to the Placental Transfer of Emtricitabine.  ANTIMICROBIAL AGENTS AND CHEMOTHERAPY,      [PMID:31160284] [10.1128/AAC.00199-19]

5. Yufeng Chen, Fan Xue, Guobin Xia, Zhenlei Zhao, Chun Chen, Yunhong Li, Ying Zhang.  (2019)  Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells.  Food & Function,  10  (8): (5215-5227).  [PMID:31384856] [10.1039/C9FO01007F]

6. Peter Yaro, Jing Nie, Mingcheng Xu, Kui Zeng, Houhong He, Jianbiao Yao, Ruwei Wang, Su Zeng.  (2019)  Influence of organic anion transporter 1/3 on the pharmacokinetics and renal excretion of ginkgolides and bilobalide.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:31325605] [10.1016/j.jep.2019.112098]

7. Bin Lin, Libin Wan, Xiaojie Sun, Chuixiu Huang, Stig Pedersen-Bjergaard, Xiantao Shen.  (2018)  Electromembrane extraction of high level substances: A novel approach for selective recovery of templates in molecular imprinting.  JOURNAL OF MEMBRANE SCIENCE,      [PMID:] [10.1016/j.memsci.2018.09.056]

8. Lili Wu, Yulian Chen, Han Liu, Zhikun Zhan, Zhi Liang, Tao Zhang, Zheng Cai, Ling Ye, Menghua Liu, Jie Zhao, Shuwen Liu, Lan Tang.  (2018)  Emodin-induced hepatotoxicity was exacerbated by probenecid through inhibiting UGTs and MRP2.  TOXICOLOGY AND APPLIED PHARMACOLOGY,      [PMID:30248416] [10.1016/j.taap.2018.09.029]

9. Liu Yixian, Wang Yafeng, Peng Youmei, Liu Bingjie, Ma Fang, Jiang Jinhua, Wang Qingduan, Chang Junbiao.  (2018)  Effects of the antiretroviral drug 2'-deoxy-2'-β-fluoro-4'-azidocytidine (FNC) on P-gp, MRP2 and BCRP expressions and functions.  PHARMAZIE,  73  (9): (503-507).  [PMID:30223932] [10.1691/ph.2018.8555]

10. Wei Li, Bi-De Liu, Kai Liao, Yong Liu, Zi-Jin Wan, Yu-Fen Dong, Qian-Qian Cao, Qian Zhu, Xiao Gu.  (2018)  Alteration of Androgen Receptor Protein Stability by Triptolide in LNCaP Cells.  Medicina-Lithuania,  54  (3): (39).  [PMID:30344270] [10.3390/medicina54030039]

11. Yixian Liu, Bingjie Liu, Yan Zhang, Youmei Peng, Chenzheng Huang, Ning Wang, Jinhua Jiang, Qingduan Wang, Junbiao Chang.  (2017)  Intestinal absorption mechanisms of 2′-deoxy-2′-β-fluoro-4′-azidocytidine, a cytidine analog for AIDS treatment, and its interaction with P-glycoprotein, multidrug resistance-associated protein 2 and breast cancer resistance protein.  EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,      [PMID:28487144] [10.1016/j.ejps.2017.05.009]

12. Wen-Hao Yu, Na Zhang, Jin-Feng Qi, Chen Sun, Yong-Hui Wang, Mei Lin.  (2015)  Arsenic and Mercury Containing Traditional Chinese Medicine (Realgar and Cinnabar) Strongly Inhibit Organic Anion Transporters, Oat1 and Oat3, In Vivo in Mice.  Biomed Research International,      [PMID:26788513] [10.1155/2015/863971]

13. Qianyi Zhang, Hongjun Zhuang, Xiaofei Wen, Yonghui Su, Jiamian Wang, Hao Qin, Jiaqian Wang, Zhaoshui Shangguan, Yiqun Ma, Jian Dong, Bo Tian, Xilei Li.  (2025)  Organelle remodeling enhances mitochondrial ATP disruption for blocking neuro-pain signaling in bone tumor therapy.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2025.159825]

14. Hang Mei, Huajing Liu, Qianqian Shang, Ying Dong, Stig Pedersen-Bjergaard, Chuixiu Huang, Xiantao Shen.  (2021)  Organic-solvent-free electromembrane extraction based on semi-interpenetrating polymer networks.  GREEN CHEMISTRY,  23  (4): (1782-1793).  [PMID:] [10.1039/D1GC00148E]

15. Hongming Tang, Tao Hou, Han Zhou, Han Liao, Fangfang Xu, Xiaomin Xie, Wenjie Yuan, Zhixin Guo, Yanfang Liu, Jixia Wang, Weijia Zhou, Xinmiao Liang.  (2024)  Label-free cell phenotypic profiling of histamine H4R receptor and discovery of non-competitive H4R antagonist from natural products.  BIOORGANIC CHEMISTRY,      [PMID:38643561] [10.1016/j.bioorg.2024.107387]

16. Yueyuan Wang, Bo Lv, Kai Fan, Cunjin Su, Delai Xu, Jie Pan.  (2024)  Metabolic Disturbances in a Mouse Model of MPTP/Probenecid-Induced Parkinson’s Disease: Evaluation Using Liquid Chromatography-Mass Spectrometry.  Neuropsychiatric Disease and Treatment,      [PMID:39220601] [10.2147/NDT.S471744]

17. Zherui Zhang, Yuhao Luo, Yuanhong Ma, Yaofeng Zhou, Dingcheng Zhu, Wanhua Shen, Junqiu Liu.  (2024)  Photocatalytic manipulation of Ca2+ signaling for regulating cellular and animal behaviors via MOF-enabled H2O2 generation.  Science Advances,  10  (16):   [PMID:38640246] [10.1126/sciadv.adl0263]

18. Sijia Lu, Quanxin Jiang, Peihui Zhou, Limin Yin, Ning Wang, Junting Xu, Qiqi Qian, Mijia Tao, Hanrui Yin, Liu Han, Yunqing Gu, Fei Gao, Junli Liu, Suzhen Chen.  (2024)  Targeting Dlat-Trpv3 pathway by hyperforin elicits non-canonical promotion of adipose thermogenesis as an effective anti-obesity strategy.  Journal of Advanced Research,      [PMID:39631519] [10.1016/j.jare.2024.11.035]

19. Meichen Liu, Yingxia Guo, Ziyi Niu, Yufeng Guo, Shuang Feng, Xiaoyan Zhang, Jiansong You, Lei Yin, Hongyu Xue, Meiyun Shi.  (2025)  Ultra-sensitive quantification of fipronil in zebrafish tissues via UPLC-MS3.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:40311485] [10.1016/j.jchromb.2025.124625]

20. Wen Peng Shan, Shi Lei Yan, Yuan Yuan Guo, Hua Ke Yang, Jing Chun Wang, Jie Xiang.  (2025)  Aerobic exercise and gut flora: a key link to improved cognitive impairment in mice with Parkinson’s disease.  Frontiers in Aging Neuroscience,      [PMID:41195080] [10.3389/fnagi.2025.1630003]

21. Meichen Liu, Yingxia Guo, Jinhe Liu, Zihan Tang, Yufeng Guo, Xintao Liu, Deshan Zhou, Lei Yin, Meiyun Shi.  (2025)  Rapid and Sensitive Quantitation of Fipronil and Its Metabolites Fipronil Sulfone, Fipronil Sulfide, and Fipronil Desulfinyl in Zebrafish Tissues by UHPLC-MS/MS.  JOURNAL OF SEPARATION SCIENCE,  48  (12): (e70326).  [PMID:41312965] [10.1002/jssc.70326]

22. Yaoyong Wang, Yifan Li, Zihan Chen, Yongchen Zhao.  (2025)  Role of the PSMC1 gene in the pathological progression of Parkinson’s disease.  American Journal of Translational Research,  17  (11): (8712).  [PMID:41415092] [10.62347/BWYD6434]

23. He-Mei Yin, Xin-Yu Sun, Ping Xu, Shu-Long Liu, Fu-Min Xue.  (2026)  The First Cocrystal of Baloxavir Marboxil: Insight to the Impact of the Unique O–H···O Hydrogen Bond on Cocrystal Structure and Properties.  CRYSTAL GROWTH & DESIGN,      [PMID:] [10.1021/acs.cgd.5c01819]