2. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Anti-infection
  3. TRP Channel
    Bacterial
    HIV
  4. Probenecid

Probenecid 

Cat. No.: HY-B0545 Purity: 99.95%
COA Handling Instructions

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.

Probenecid Chemical Structure

Probenecid Chemical Structure

CAS No. : 57-66-9

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10 mM * 1 mL in DMSO USD 61 In-stock
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Probenecid:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

IC50 & Target

TRPV2[1]
In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Administration of Probenecid to WT mice results in increased contractility as measured via ejection fraction (EF) relative to EF in control mice given saline. The increased contractility is noted within 5 minutes of the bolus injection with all doses at or above 75 mg/kg (peak change of 5.26±3.35, 8.40±2.80, 7.32±2.52 for 75mg/kg, 100mg/kg and 200mg/kg, respectively). The measured change in contractility as measured at 5 minute intervals (for 30 minutes total) revealed a dose dependent increase in contractility with an estimated EC50 of 49.33 mg/kg. The EF remained at an elevated state for at least 1 hour on subjects (n=5, dose of 200 mg/kg IV) that are evaluated for a longer period of time (average increase in EF over baseline of 8.9±2.57)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

285.36

Appearance

Solid

Formula

C13H19NO4S
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (350.43 mM)

0.5 M NaOH : 100 mg/mL (350.43 mM; ultrasonic and adjust pH to 12 with NaOH)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5043 mL 17.5217 mL 35.0435 mL
5 mM 0.7009 mL 3.5043 mL 7.0087 mL
10 mM 0.3504 mL 1.7522 mL 3.5043 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.95%

COA (252 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Probenecid57-66-9TRP ChannelBacterialHIVTransient receptor potential channelsHuman immunodeficiency virusInhibitorinhibitorinhibit

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