1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter

AR-C155858 (Synonyms: AR C155858)

Cat. No.: HY-13248 ee.: 99.30%
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

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

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.

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

ee.: 99.30%

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Product Name:
AR-C155858
Cat. No.:
HY-13248
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