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

AR-C155858 

Cat. No.: HY-13248
Handling Instructions

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
10 mM * 1 mL in DMSO USD 378 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 372 In-stock
Estimated Time of Arrival: December 31
10 mg USD 624 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1824 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

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

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

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    • References

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    Description

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

    IC50 & Target

    Ki: 2.3 nM (MCT1), 10 nM (MCT2)

    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].

    Molecular Weight

    461.53

    Formula

    C₂₁H₂₇N₅O₅S

    CAS No.

    496791-37-8

    SMILES

    O=C(C1=C2SC(CC3=C(NN=C3C)C)=C1C(N4C[[email protected]@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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (108.34 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2167 mL 1.0834 mL 2.1667 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: ≥ 2.75 mg/mL (5.96 mM); Clear solution

    • 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

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    AR-C155858Monocarboxylate TransporterInhibitorinhibitorinhibit

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