Probenecid
Based on 49 publication(s) in Google Scholar
Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 57-66-9
- Formula: C13H19NO4S
- Molecular Weight:285.36
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Probenecid
More- Cell Res. 2022 Jul;32(7):638-658. [Abstract]
- Immunity. 2022 Apr 12;55(4):686-700.e7. [Abstract]
- Nat Immunol. 2026 May;27(5):949-960. [Abstract]
- Cell Mol Immunol. 2020 Mar;17(3):261-271. [Abstract]
- Nat Commun. 2026 May 5;17(1):6063. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Adv Sci (Weinh). 2025 Dec 22:e09056. [Abstract]
- Adv Sci (Weinh). 2025 Oct 6:e10270. [Abstract]
- Adv Sci (Weinh). 2025 Jul;12(28):e2503579. [Abstract]
- Cell Death Differ. 2026 Mar 31. [Abstract]
- Int J Biol Sci. 2022 Apr 11;18(7):2914-2931. [Abstract]
- Acta Pharmacol Sin. 2025 Sep 15. [Abstract]
- J Transl Med. 2025 Jul 11;23(1):781. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Food Res Int. 2025 Feb:201:115590. [Abstract]
- Drug Deliv. 2025 Dec;32(1):2490269. [Abstract]
- Cell Rep. 2025 Mar 25;44(4):115466. [Abstract]
- Chin Med. 2026 Jan 24;21(1):51. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Front Immunol. 2026 Jan 12:16:1683500. [Abstract]
- Redox Rep. 2026 Dec 31;31(1):2668238. [Abstract]
- J Agric Food Chem. 2016 Oct 26;64(42):7899-7910. [Abstract]
- Biochem Pharmacol. 2026 Jun 12;251(Pt 2):118159. [Abstract]
- Transl Res. 2024 May 9:271:26-39. [Abstract]
- Pharmaceuticals (Basel). 2026 May;19(5):711. [Abstract]
- Int J Mol Sci. 2019 Mar 5;20(5):1125. [Abstract]
- Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]
- Chem Biol Interact. 2025 Jan 5:405:111293. [Abstract]
- Cell Calcium. 2026 Mar 20:135:103133. [Abstract]
- Cell Calcium. 2024 Jun:120:102883. [Abstract]
- Exp Neurol. 2025 Jan:383:115040. [Abstract]
- Regul Toxicol Pharmacol. 2019 Nov:108:104449. [Abstract]
- J Endocrinol Invest. 2025 Feb;48(2):317-332. [Abstract]
- Toxicol Appl Pharmacol. 2024 Nov:492:117112. [Abstract]
- Neuroscience. 2022 Jul 1:494:51-68. [Abstract]
- Mol Pharmacol. 2025 Dec;107(12):100084. [Abstract]
- J Dig Dis. 2025 Apr 14. [Abstract]
- Toxicol In Vitro. 2020 Dec:69:104971. [Abstract]
- Adv Med Educ Pract. 2021 Mar 4:12:237-243. [Abstract]
- Biochem Biophys Res Commun. 2024 Aug 20:721:150128. [Abstract]
- Biopharm Drug Dispos. 2022 Dec;43(6):265-271. [Abstract]
- Lasers Surg Med. 2017 Sep;49(7):719-726. [Abstract]
- Cutan Ocul Toxicol. 2026 Jun;45(2):243-250. [Abstract]
- bioRxiv. 2026 Mar 12.
- bioRxiv. 2026 Jan 7.
- bioRxiv. 2025 Dec 18.
- Res Sq. 2024 Nov 17.
- Research Square Print. August 31st, 2022.
- Research Square Preprint. 2021 Aug.
Biological Activity
|
TRPV2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
6.3 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells
TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells
|
[PMID: 10929807] |
| CHO | IC50 |
7.4 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
|
[PMID: 10991954] |
| CHO | IC50 |
3.02 μM
Compound: probenecid
|
Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins
Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins
|
[PMID: 23344796] |
| CHO | EC50 |
4.2 mM
Compound: Probenecid
|
Agonist activity at human TRPA1 expressed in CHO cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay
Agonist activity at human TRPA1 expressed in CHO cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay
|
[PMID: 30878828] |
| HEK293 | IC50 |
50 μM
Compound: probenecid
|
Inhibition of human URAT1-mediated urate uptake in HEK293 cells
Inhibition of human URAT1-mediated urate uptake in HEK293 cells
|
[PMID: 17325024] |
| S2 | IC50 |
12.5 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cells
TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cells
|
[PMID: 12472777] |
| S2 | IC50 |
12.3 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
|
[PMID: 14978359] |
| S2 | IC50 |
25.4 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
|
[PMID: 14978359] |
| S2 | IC50 |
4.93 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
|
[PMID: 14978359] |
| S2 | IC50 |
6.03 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
|
[PMID: 14978359] |
| S2 | IC50 |
668 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of PGF2alpha uptake (PGF2: 50nM) in hOAT2-expressing S2 cells
TP_TRANSPORTER: inhibition of PGF2alpha uptake (PGF2: 50nM) in hOAT2-expressing S2 cells
|
[PMID: 14978359] |
| S2 | IC50 |
977 μM
Compound: Probenecid
|
TP_TRANSPORTER: inhibition of PGF2alpha uptake (PGF2: 50nM) in rOAT2-expressing S2 cells
TP_TRANSPORTER: inhibition of PGF2alpha uptake (PGF2: 50nM) in rOAT2-expressing S2 cells
|
[PMID: 14978359] |
| Sf21 | IC50 |
509.9 μM
Compound: Probenecid
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| Sf21 | IC50 |
564.8 μM
Compound: Probenecid
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
Probenecid efficiently inhibits ATP-dependent active vesicular N-ethylmaleimide glutathione (NEM-GS) uptake by both MRP1 and MRP2. A significant inhibition of the MRP1-ATPase is observed at higher organic anion concentrations. In contrast, the ATPase activity of MRP2 is strongly stimulated by both Probenecid (approximate KACT=250 μM), sulfinpyrazone (KACT=300 μM), and indomethacin (KACT=150 μM), and ATPase activation is even stronger than in the case of NEM-GS. The organic anion activation of the MRP2-ATPase followed bell-shaped curves, with maximum values obtained at about 2 mM for Probenecid, 800 μM for sulfinpyrazone, and 400 μM for indomethacin[2]. Probenecid is an inhibitor of the hTAS2R16, hTAS2R38, and hTAS2R43 bitter taste receptors. Probenecid acts on a subset of TAS2Rs and inhibits through a novel, allosteric mechanism of action. Probenecid is also commonly used to enhance cellular signals in GPCR calcium mobilization assays. Probenecid specifically inhibits the cellular response mediated by the bitter taste receptor hTAS2R16 and provide molecular and pharmacological evidence for direct interaction with this GPCR using a non-competitive (allosteric) mechanism[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 57-66-9
-
Appearance Solid
-
Molecular Weight 285.36
-
Formula C13H19NO4S
-
Color White to off-white
-
SMILES
O=C(O)C1=CC=C(S(=O)(N(CCC)CCC)=O)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (49)
-
Journal Impact Factor
-
Most Recent
-
Cell Res
SLC1A1-mediated cellular and mitochondrial influx of R-2-hydroxyglutarate in vascular endothelial cells promotes tumor angiogenesis in IDH1-mutant solid tumors. [Abstract]2022 Jul;32(7):638-658. PMID: 35459936 -
Immunity
Intestinal Tuft-2 cells exert antimicrobial immunity via sensing bacterial metabolite N-undecanoylglycine. [Abstract]2022 Apr 12;55(4):686-700.e7. PMID: 35320705 -
Nat Immunol
Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. [Abstract]2026 May;27(5):949-960. PMID: 41781710 -
Cell Mol Immunol
ACPAs promote IL-1β production in rheumatoid arthritis by activating the NLRP3 inflammasome. [Abstract]2020 Mar;17(3):261-271. PMID: 30911117 -
Nat Commun
ERα blockade in dendritic cells enhances antigen cross-presentation and induces antitumor CD8+ T cell immunity. [Abstract]2026 May 5;17(1):6063. PMID: 42086580 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Adv Sci (Weinh)
Hyperviscous Diabetic Bone Marrow Niche Impairs BMSCs Osteogenesis via TRPV2-Mediated Cytoskeletal-Nuclear Mechanotransduction. [Abstract]2025 Dec 22:e09056. PMID: 41431162 -
Adv Sci (Weinh)
Uric Acid Functions as an Endogenous Modulator of Microglial Function and Amyloid Clearance in Alzheimer's Disease. [Abstract]2025 Oct 6:e10270. PMID: 41051385 -
Adv Sci (Weinh)
Neuronal FGF13 Inhibits Mitochondria-Derived Damage Signals to Prevent Neuroinflammation and Neurodegeneration in a Mouse Model of Parkinson's Disease. [Abstract]2025 Jul;12(28):e2503579. PMID: 40344619 -
Cell Death Differ
2026 Mar 31. PMID: 41917182 -
Int J Biol Sci
GRP75-faciliated Mitochondria-associated ER Membrane (MAM) Integrity controls Cisplatin-resistance in Ovarian Cancer Patients. [Abstract]2022 Apr 11;18(7):2914-2931. PMID: 35541901 -
Acta Pharmacol Sin
Species differences in the hepatobiliary disposition of morphine-6-glucuronide mediated by hepatic transporters in rats and humans. [Abstract]2025 Sep 15. PMID: 40954191 -
J Transl Med
Chronic sleep deprivation induces plasma exosome-derived miR-150-5p downregulation as a novel mechanism involved in Parkinson's disease progression by targeting DCLK1. [Abstract]2025 Jul 11;23(1):781. PMID: 40646516 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Food Res Int
Ergothioneine exerts neuroprotective effects in Parkinson's disease: Targeting α-synuclein aggregation and oxidative stress. [Abstract]2025 Feb:201:115590. PMID: 39849723 -
Drug Deliv
Reliable high-PAP-1-loaded polymeric micelles for cancer therapy: preparation, characterization, and evaluation of anti-tumor efficacy. [Abstract]2025 Dec;32(1):2490269. PMID: 40207975 -
Cell Rep
Structural basis for the reversal of human MRP4-mediated multidrug resistance by lapatinib. [Abstract]2025 Mar 25;44(4):115466. PMID: 40138312 -
Chin Med
Targeting G-protein-coupled receptors and gut microbiota: Ge-Lian Qi-Shen decoction elevates GLP-1 to combat non-alcoholic fatty liver disease. [Abstract]2026 Jan 24;21(1):51. PMID: 41580820 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Front Immunol
TENS alleviates CP/CPPS-related inflammation and pain by modulating Kir2.1-dependent macrophage polarization. [Abstract]2026 Jan 12:16:1683500. PMID: 41624842 -
Redox Rep
Uric acid alleviates the inflammatory response in LPS-induced BV2 cells and MPTP-induced PD mice by resisting ferroptosis through the Nrf2 signalling pathway. [Abstract]2026 Dec 31;31(1):2668238. PMID: 42241031 -
J Agric Food Chem
Nuciferine Alleviates Renal Injury by Inhibiting Inflammatory Responses in Fructose-Fed Rats. [Abstract]2016 Oct 26;64(42):7899-7910. PMID: 27718563 -
Biochem Pharmacol
Aquaporin-1 (AQP1) mediates cardiac oedema and mitochondrial dysfunction in cardiometabolic HFpEF: New insights into the mechanisms of SGLT2 inhibitors. [Abstract]2026 Jun 12;251(Pt 2):118159. PMID: 42285370 -
Transl Res
Counteracting TGM2 by a Fibroin peptide ameliorated Adriamycin-induced nephropathy via regulation of lipid metabolism through PANX1-PPAR α/PANK1 pathway. [Abstract]2024 May 9:271:26-39. PMID: 38734063 -
Pharmaceuticals (Basel)
Neuroprotective Effects of Rosa roxburghii Tratt Juice Concentrate Powder in Parkinson's Disease Mice via the PI3K/AKT Signaling Pathway. [Abstract]2026 May;19(5):711. PMID: 42198384 -
Int J Mol Sci
Cisplatin Synergistically Enhances Antitumor Potency of Conditionally Replicating Adenovirus via p53 Dependent or Independent Pathways in Human Lung Carcinoma. [Abstract]2019 Mar 5;20(5):1125. PMID: 30841620 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Chem Biol Interact
7-Hydroxycoumarin and its conjugated metabolites interact with organic anion transporters 1 and 3 in vitro and in vivo. [Abstract]2025 Jan 5:405:111293. PMID: 39481674 -
Cell Calcium
Impact of channel properties, imaging strategies and diffusional constraints on the detectability of Ca2+ microdomains. [Abstract]2026 Mar 20:135:103133. PMID: 41895149 -
Cell Calcium
Simultaneous TIRF imaging of subplasmalemmal Ca2+ dynamics and granule fusions in insulin-secreting INS-1 cells reveals coexistent synchronized and asynchronous release. [Abstract]2024 Jun:120:102883. PMID: 38643716 -
Exp Neurol
Early α-synuclein/synapsin III co-accumulation, nigrostriatal dopaminergic synaptopathy and denervation in the MPTPp mouse model of Parkinson's Disease. [Abstract]2025 Jan:383:115040. PMID: 39500391 -
Regul Toxicol Pharmacol
2019 Nov:108:104449. PMID: 31449916 -
J Endocrinol Invest
2025 Feb;48(2):317-332. PMID: 39527372 -
Toxicol Appl Pharmacol
Human trophoblast organoids for improved prediction of placental ABC transporter-mediated drug transport. [Abstract]2024 Nov:492:117112. PMID: 39326791 -
Neuroscience
Inhibition of TRPA1 Attenuates Oxidative Stress-induced Damage After Traumatic Brain Injury via the ERK/AKT Signaling Pathway. [Abstract]2022 Jul 1:494:51-68. PMID: 35158017 -
Mol Pharmacol
Transient receptor potential vanilloid 3 activation accelerates keratinocyte migration in vitro but not dermal wound healing in vivo. [Abstract]2025 Dec;107(12):100084. PMID: 41240425 -
J Dig Dis
DREADDs-Based Chemogenetics Induced Slow Transit Constipation via Inhibition of Enteric Neurons. [Abstract]2025 Apr 14. PMID: 40223443 -
Toxicol In Vitro
YAN, a novel microtubule inhibitor, inhibits P-gp and MRP1 function and induces mitotic slippage followed by apoptosis in multidrug-resistant A549/Taxol cells. [Abstract]2020 Dec:69:104971. PMID: 32805372 -
Adv Med Educ Pract
Online Medical Education in India - Different Challenges and Probable Solutions in the Age of COVID-19. [Abstract]2021 Mar 4:12:237-243. PMID: 33692645 -
Biochem Biophys Res Commun
Protective role of TRPV2 in synaptic plasticity through the ERK1/2-CREB-BDNF pathway in chronic unpredictable mild stress rats. [Abstract]2024 Aug 20:721:150128. PMID: 38776831 -
Biopharm Drug Dispos
Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells. [Abstract]2022 Dec;43(6):265-271. PMID: 36195987 -
Lasers Surg Med
The sensitivity of glioma cells to pyropheophorbide-αmethyl ester-mediated photodynamic therapy is enhanced by inhibiting ABCG2. [Abstract]2017 Sep;49(7):719-726. PMID: 28370217 -
Cutan Ocul Toxicol
Leveraging a TRPV1-overexpressing cell model: an integrated testing strategy for UV filter-induced ocular irritation. [Abstract]2026 Jun;45(2):243-250. PMID: 41985167 -
-
-
-
-
-
Solvent & Solubility
DMSO : ≥ 100 mg/mL (350.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.5 M NaOH : 100 mg/mL (350.43 mM; ultrasonic and adjust pH to 12 with NaOH)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 5% Sodium bicarbonate in ddH2O
Solubility: 16 mg/mL (56.07 mM); Clear solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.76 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
HEK-293T cells are transfected with hTAS2R expression constructs using Lipofectamine 2000 in poly-lysine coated, black 384-well plates with clear bottoms and incubated for 22 hours at 37°C. Growth media is removed and cells are washed twice with HBSS containing 20 mM HEPES, then loaded with a calcium indicator dye in HBSS containing 20 mM HEPES (Calcium 4 Assay kit) with or without 1 mM Probenecid. Cells are incubated at 37°C for 1 hour in the presence of both dye and Probenecid, then moved to a Flexstation II-384 set for 32°C. After a 15-minute temperature equilibration (without washout), indicated compounds are injected (at t=~25 seconds) and fluorescence is measured for 100 to 180 seconds, reading every 3 seconds. Data sets are analyzed and represented as % over baseline signal using Prism 5.0 software. For Schild plots, replicates of raw calcium flux values are expressed as % over baseline signal. The mean value at 36 seconds (corresponding to the maximum flux signal) for each concentration of TAS2R ligand in the presence of the indicated concentration of Probenecid is plotted against the log of ligand concentration. Data points are fit using non-linear regression in GraphPad Prism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1] In order to obtain a dose response curve, male C57 WT (n=39) mice 12-16 weeks of age are anesthetized with isoflurane while intravenous jugular access (IV) is obtained under a microscope. Subsequently, an echocardiographic study with both M-mode and B-mode is obtained in parasternal long axis (PSLAX) as described below. Either saline or different doses of Probenecid (increasing from 2 to 200mg/kg) are injected (bolus IV) for the initial contractility studies in WT mice.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (284 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
-
Handling Instructions (2659 KB)
References
[1]. Koch SE, et al. Probenecid: novel use as a non-injurious positive inotrope acting via cardiac TRPV2 stimulation. J Mol Cell Cardiol. 2012 Jul;53(1):134-44. [Content Brief]
[2]. Bakos E, et al. Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. [Content Brief]
[3]. Greene TA, et al. Probenecid inhibits the human bitter taste receptor TAS2R16 and suppresses bitter perception of salicin. PLoS One. 2011;6(5):e20123. [Content Brief]
[4]. Silverman W, et al. Probenecid, a gout remedy, inhibits pannexin 1 channels. Am J Physiol Cell Physiol. 2008 Sep;295(3):C761-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 0.5 M NaOH | 1 mM | 3.5043 mL | 17.5217 mL | 35.0435 mL | 87.6086 mL |
| 5 mM | 0.7009 mL | 3.5043 mL | 7.0087 mL | 17.5217 mL | |
| 10 mM | 0.3504 mL | 1.7522 mL | 3.5043 mL | 8.7609 mL | |
| 15 mM | 0.2336 mL | 1.1681 mL | 2.3362 mL | 5.8406 mL | |
| 20 mM | 0.1752 mL | 0.8761 mL | 1.7522 mL | 4.3804 mL | |
| 25 mM | 0.1402 mL | 0.7009 mL | 1.4017 mL | 3.5043 mL | |
| 30 mM | 0.1168 mL | 0.5841 mL | 1.1681 mL | 2.9203 mL | |
| 40 mM | 0.0876 mL | 0.4380 mL | 0.8761 mL | 2.1902 mL | |
| 50 mM | 0.0701 mL | 0.3504 mL | 0.7009 mL | 1.7522 mL | |
| 60 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4601 mL | |
| 80 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0951 mL | |
| 100 mM | 0.0350 mL | 0.1752 mL | 0.3504 mL | 0.8761 mL |