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Purity: ≥98%
Probenecid (Benemid; Probecid; Benecid; Benuryl; Probenecid Martec; Probalan) is an OAT (organic anion transport) inhibitor which has been used as a medication to increase uric acid excretion in the urine. It is mainly used for the treatment of gout and hyperuricemia. Probenecid is also a TRPV2 (transient receptor potential vanilloid 2) agonist and an inhibitor of TAS2R16. Probenecid has also been used to treat patients with renal impairment as it reduces the renal tubular excretion of other drugs.
| ln Vitro |
Probenecid potently inhibits the absorption of ATP-dependent active vesicles N-ethylmaleimide glutathione (NEM-GS) by MRP1 and MRP2. Significant inhibition of MRP1-ATPase was seen at increasing organic anion concentrations. The ATPase activity of MRP2 is influenced by probenecid (about KACT=250 μM), sulfinpyrazone (KACT=300 μM) and indomethacin (KACT=150 μM), and the ATPase activation is even stronger than that of NEM-GS. Activation of MRP2-ATPase by organic anions follows a bell-shaped curve, with maximum values at 2 mM for Probenecid, 800 μM for sulfinpyrazone, and 400 μM for indomethacin [2]. Probenecid is an inhibitor of hTAS2R16, hTAS2R38 and hTAS2R43 bitter taste receptors. Probenecid operates on a subset of TAS2R and suppresses through a new allosteric mechanism of action. Probenecid is also often utilized to improve cell signaling in GPCR calcium mobilization experiments. Probenecid specifically suppresses cellular responses mediated by the bitter taste receptor hTAS2R16 and provides molecular and pharmacological evidence for direct contact with this GPCR using a non-competitive (allosteric) mechanism [3].
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| ln Vivo |
When compared to control mice fed saline, probenecid increased the contractility of WT mice as indicated by their ejection fraction (EF). At all doses of 75 mg/kg and higher, increased contractility was observed within 5 minutes of the bolus (peak changes at 75 mg/kg, 100 mg/kg, and 200 mg/kg were 5.26±3.35, 8.40±2.80, and 7.32± 2.52, respectively). With an estimated EC50 of 49.33 mg/kg, changes in contractility assessed at 5-minute intervals for a total of 30 minutes showed a dose-dependent increase in contractility. EF stayed raised for at least an hour in patients examined over a longer duration (n=5 at 200 mg/kg IV) (mean increase in EF from baseline 8.9±2.57) [1].
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| References |
Cell Calcium.1989 Apr;10(3):171-80;Cardiovasc Toxicol.2012 Mar;12(1):1-9.
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| Molecular Formula |
C13H19NO4S
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| Molecular Weight |
285.36
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| CAS # |
57-66-9
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| Related CAS # |
Probenecid;57-66-9
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| SMILES |
S(C1C([H])=C([H])C(C(=O)O[H])=C([H])C=1[H])(N(C([H])([H])C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])[H])(=O)=O
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| InChi Key |
DBABZHXKTCFAPX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19NO4S/c1-3-9-14(10-4-2)19(17,18)12-7-5-11(6-8-12)13(15)16/h5-8H,3-4,9-10H2,1-2H3,(H,15,16)
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| Chemical Name |
4-(dipropylsulfamoyl)benzoic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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