Name: Probenecid
Brand: Selleck Chemicals
SKU: S4022
Availability: InStock
Rating: 5 (4 reviews)

Jump to

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor ATPase GluR
Other TRP Channel Inhibitors	2-APB (2-Aminoethyl Diphenylborinate) SKF96365 AMG-517 GSK2193874 GSK1016790A Capsazepine HC-030031 EIPA (L593754) HC-067047 SB705498

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.400mg/ml (4.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.400mg/ml (4.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	285.36	Formula	C₁₃H₁₉NO₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	57-66-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Benemid			Smiles	CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	organic anion transport TRPV2 TAS2R16
In vitro	Probenecid is able to prevent the efflux of calcium-sensitive fluorescent dyes during studies of cellular calcium mobilization. This compound (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. It is a potent transient receptor potential vanilloid 2 (TRPV2) agonist. This chemical selectively induces increase in intracellular Ca²⁺ influx in HEK293T cells transiently expressing exogenous TRPV2. It is able to interact with organic anion transporters (OAT). 0.1 mM of this compound 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, it stimulates ATPase activity of MRP2 with approximate KACT of 250 μM, but inhibits ATPase activity of MRP1. This chemical is an inhibitor of the hTAS2R16, hTAS2R38, and hTAS2R43 bitter taste receptors. 1 mM of it attenuates saccharin-induced calcium flux responses of hTAS2R16 to near baseline levels. It 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 its activity as a transport inhibitor, but is concerning with its interaction with the receptor.
In vivo	Probenecid is an inhibitor of organic transport in vivo. This compound is able to decrease the renal clearance of antibiotic, such as penicillin, which enhances serum levels of antibiotic. It 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. This chemical 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/2720761/ [2] https://pubmed.ncbi.nlm.nih.gov/17850966/ [3] https://pubmed.ncbi.nlm.nih.gov/10727523/ [4] https://pubmed.ncbi.nlm.nih.gov/21629661/ [5] https://pubmed.ncbi.nlm.nih.gov/21938493/ [6] https://pubmed.ncbi.nlm.nih.gov/18596212/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04939623	Recruiting	Chronic Pain\|Drug Dependence of Morphine Type\|Symptom Withdrawal	University of Calgary	October 31 2023	Phase 2
NCT05497674	Completed	Type 2 Diabetes Mellitus	Sunshine Lake Pharma Co. Ltd.	February 21 2022	Phase 1
NCT05082909	Unknown status	Infection Bacterial	Imperial College London	December 21 2021	Phase 1\|Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Probenecid TRP Channel agonist

Chemical Structure

Molecular Weight: 285.36