[CAS NO. 496791-37-8] AR-C155858

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Catalog:	HY-13248
Brand:	MCE
CAS:	496791-37-8

Overview

MDL	MFCD22124476
Molecular Weight	461.53
Molecular Formula	C21H27N5O5S
SMILES	O=C(C1=C2SC(CC3=C(NN=C3C)C)=C1C(N4C[C@@H](CO4)O)=O)N(C(N2CC(C)C)=O)C

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

28 Publications Citing Use of MCE

[1]Cell Metab. 2019 Mar 5;29(3):668-680.e4.
[2]Sci Adv. 2022 Sep 16;8(37):eabo7639.
[3]Nat Commun. 2020 May 15;11(1):2429.
[4]Proc Natl Acad Sci U S A. 2015 Sep 1;112(35):11090-5.
[5]Theranostics. 2020 Jul 9;10(18):8430-8445.
[6]Cell Rep. 2021 Jan 19;34(3):108642.
[7]Glia. 2018 Oct;66(10):2233-2245.
[8]J Neurosci. 2015 Mar 11;35(10):4168-78.
[9]J Cell Physiol. 2017 Jan;232(1):136-44.
[10]Oncol Res. 2022 Feb 7.
[11]Front Oncol. 2022 Jul 28;12:960066.
[12]Crit Rev Anal Chem. 2021 Mar 10;1-15.
[13]Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C116-26.
[14]J Biol Chem. 2018 Oct 12;293(41):16019-16027.
[15]AAPS J. 2019 Jan 7;21(2):13.
[16]AAPS J. 2018 Nov 5;21(1):3.
[17]J Pharmacol Exp Ther. 2019 Jul;370(1):84-91.
[18]Pharm Res. 2019 Dec 10;37(1):5.
[19]Pharm Res. 2015 Jun;32(6):1894-906.
[20]J Pharm Biomed Anal. 2018 Jun 5;155:270-275.
[21]PLoS One. 2016 Apr 7;11(4):e0153135.
[22]PLoS One. 2014 Jan 21;9(1):e85780.
[23]PLoS One. 2013;8(2):e57712.
[24]J Pharm Pharmacol. 2014 Apr;66(4):574-83.
[25]bioRxiv. November 19, 2021.
[26]Research Square Preprint. 2021 Feb.
[27]Medicine, University of Berlin. 2019 Feb
[28]Oncotarget. 2014 Nov 30;5(22):11029-37.

Summary

AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with K _i s 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 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] .

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

Appearance

Solid

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 available by MCE.

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.
[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.
[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.

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