1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter

AR-C155858 (Synonyms: AR C155858)

Cat. No.: HY-13248 Purity: 95.09% ee.: 99.30%
Data Sheet SDS Handling Instructions

AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

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AR-C155858 Chemical Structure

AR-C155858 Chemical Structure

CAS No. : 496791-37-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO $315 In-stock
1 mg $110 In-stock
5 mg $310 In-stock
10 mg $520 In-stock
50 mg $1520 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

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Description

AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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]

AR-C155858 is dissolved in DMSO.

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
M.Wt

461.53

Formula

C₂₁H₂₇N₅O₅S

CAS No.

496791-37-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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AR-C155858
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HY-13248
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