2. Membrane Transporter/Ion Channel
  3. Monocarboxylate Transporter
  4. AR-C155858

AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.

For research use only. We do not sell to patients.

AR-C155858 Chemical Structure

AR-C155858 Chemical Structure

CAS No. : 496791-37-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 378 In-stock
Solution
10 mM * 1 mL in DMSO USD 378 In-stock
Solid
1 mg USD 132 In-stock
5 mg USD 372 In-stock
10 mg USD 624 In-stock
50 mg USD 1824 In-stock
100 mg USD 2600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 40 publication(s) in Google Scholar

AR-C155858 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE AR-C155858

Proliferation Assay

    AR-C155858 purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C116-26.  [Abstract]

    Inhibition of pyruvate transport in HEK293 cells. Summary of 24 cells in three separate experiments.

    AR-C155858 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 Nov 30;5(22):11029-37.  [Abstract]

    The MCT1/2 inhibitor AR-C155858 significantly reduces mammosphere formation in MDA-MB-231 cells. Note that AR-C155858 also effectively reduces mammosphere formation in this cellular context, with an IC50 of ~1-2 μM. The vehicle-alone control is normalized to one.

    View All Monocarboxylate Transporter Isoform Specific Products:

    View All Isoforms
    MCT1 MCT2 MCT4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.

    IC50 & Target

    MCT1

     

    MCT2

     

    Cellular Effect
    Cell Line Type Value Description References
    Raji EC50
    18 nM
    Compound: 2
    Growth inhibition of human Raji cells after 96 hrs by MTT assay
    Growth inhibition of human Raji cells after 96 hrs by MTT assay
    		[PMID: 25068893]
    In Vitro

    AR-C155858 (10 nM-100 nM) inhibits MCT1/MCT2 C-terminal chimaeras[1]. AR-C155858 inhibits MCT2, and the 70% inhibition seen at 10 nM is followed by a gradually increasing inhibition which can only be explained by a Ki value of significantly less than 10 nM. AR-C155858 inhibits MCT1 expressed in Xenopus oocytes in a time- and concentration-dependent manner[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    AR-C155858 Related Antibodies
    Molecular Weight

    461.53

    Formula

    C21H27N5O5S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=C2SC(CC3=C(NN=C3C)C)=C1C(N4C[C@@H](CO4)O)=O)N(C(N2CC(C)C)=O)C
    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
    Solvent & Solubility
    In Vitro: 

    DMSO : 70 mg/mL (151.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1667 mL 10.8335 mL 21.6671 mL
    5 mM 0.4333 mL 2.1667 mL 4.3334 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.75 mg/mL (5.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (5.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.62%

    SDS (252 KB)

    COA (258 KB) HNMR (196 KB) LCMS (93 KB)

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

    MCT kinetic assays are performed by monitoring intracellular pH with H+-sensitive dye BCECF or by determining the uptake of l-[14C]lactate (7.4 MBq/mL). The uptake buffer containes 75 mM NaCl, 2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Tris/Hepes (pH 7.4). AR-C155858 inhibitor titrations are performed at pH 6 with oocytes preincubated for 45 min in a different uptake buffer (75 mM NaCl, 2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Mes, pH 6) containing the required concentration of AR-C155858 prior to measuring the uptake of l-[14C]lactate (0.5 mM). Unless stated otherwise, uptake is determined over 2.5 min for all MCT constructs except for MCT2trn with or without embigin and MCT2/1 with or without embigin, where 5 and 10 min are used respectively.

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

    The erythrocytes (5% haematocrit) are pre-incubated for 1 h at room temperature (22°C) with or without AR-C155858 at the required concentration before assaying transport of l-lactate (10 mM) at 6°C. Initial rates of transport are calculated by first-order regression analysis of the time course of pH change and converted into nmol of H+/min by determining the pH change induced by small additions of standardized NaOH.

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

    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 1 mM 2.1667 mL 10.8335 mL 21.6671 mL 54.1677 mL
    5 mM 0.4333 mL 2.1667 mL 4.3334 mL 10.8335 mL
    10 mM 0.2167 mL 1.0834 mL 2.1667 mL 5.4168 mL
    15 mM 0.1444 mL 0.7222 mL 1.4445 mL 3.6112 mL
    20 mM 0.1083 mL 0.5417 mL 1.0834 mL 2.7084 mL
    25 mM 0.0867 mL 0.4333 mL 0.8667 mL 2.1667 mL
    30 mM 0.0722 mL 0.3611 mL 0.7222 mL 1.8056 mL
    40 mM 0.0542 mL 0.2708 mL 0.5417 mL 1.3542 mL
    50 mM 0.0433 mL 0.2167 mL 0.4333 mL 1.0834 mL
    60 mM 0.0361 mL 0.1806 mL 0.3611 mL 0.9028 mL
    80 mM 0.0271 mL 0.1354 mL 0.2708 mL 0.6771 mL
    100 mM 0.0217 mL 0.1083 mL 0.2167 mL 0.5417 mL
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    AR-C155858 Related Classifications

    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.

    Keywords:

    AR-C155858496791-37-8Monocarboxylate TransporterInhibitorinhibitorinhibit

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