[CAS NO. 496791-37-8] AR-C155858
PRODUCTS SPECIFICATIONS [496791-37-8]
DESCRIPTION [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 |
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
DMSO : ≥ 50 mg/mL ( 108.34 mM )
* "≥" means soluble, but saturation unknown.
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 |
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1.
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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
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.