HY-13248-1mg | AR-C155858 [496791-37-8] Biotrend USA

Description

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

IC₅₀ & Target

MCT1

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 K_i 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.

Molecular Weight

461.53

Formula

C₂₁H₂₇N₅O₅S

CAS No.

496791-37-8

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
10 mM	0.2167 mL	1.0834 mL	2.1667 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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)

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%

Select Batch:

Data Sheet (283 KB) SDS (0 KB)

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

Handling Instructions (2659 KB)

References

[1]. Ovens MJ, et al. The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem J. 2010 Oct 15;431(2):217-25. [Content Brief]

[2]. Ovens MJ, et al. AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem J. 2010 Jan 15;425(3):523-30. [Content Brief]

[3]. Vijay N, et al. A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose. Pharm Res. 2015 Jun;32(6):1894-906. [Content Brief]

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	[1]. Ovens MJ, et al. The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem J. 2010 Oct 15;431(2):217-25. [Content Brief] [2]. Ovens MJ, et al. AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem J. 2010 Jan 15;425(3):523-30. [Content Brief] [3]. Vijay N, et al. A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose. Pharm Res. 2015 Jun;32(6):1894-906. [Content Brief]

Complete Stock Solution Preparation Table

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

AR-C155858 [496791-37-8]

Cat# HY-13248-1mg

Brand : MedChemExpress

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AR-C155858 Related Classifications

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AR-C155858 [496791-37-8]

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Brand : MedChemExpress

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AR-C155858 Related Classifications

Keywords:

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