AR-C155858 |
Catalog No.GC10680
One-Click Copy Product Info
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AR-C155858 es un potente inhibidor del transportador de monocarboxilato 1 (MCT1) con un valor de Ki de 2.3nM, y también inhibe MCT2 con un valor de Ki de >10nM
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 496791-37-8
Sample solution is provided at 25 µL, 10mM.
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AR-C155858 es un potente inhibidor del transportador de monocarboxilato 1 (MCT1) con un valor de Ki de 2.3nM, y también inhibe MCT2 con un valor de Ki de >10nM[1]. AR-C155858 tiene posibles propiedades inmunomoduladoras y quimioterapéuticas [2, 3]. MCT1 se expresa en la mayoría de los tejidos y promueve la absorción de lactato para la oxidación en el músculo cardíaco y esquelético rojo, así como la gluconeogénesis en el hígado y el riñón de algunas especies[4]. AR-C155858 puede inhibir la proliferación, la migración, la formación de esferoides y el crecimiento tumoral in vivo de las células TAMR-MCF-7 [5].
In vitro, el tratamiento de células de cáncer de mama 4T1 con AR-C155858 (0-500nM) durante 48h inhibió el crecimiento celular de una manera dependiente de la concentración con un valor de IC50 de 20.3nM, inhibiendo la absorción celular de L-lactate[6].
In vivo, AR-C155858 (5mg/kg) administrado por vía intravenosa a ratas coadministradas con γ-hydroxybutyrate (GHB) y etanol redujo significativamente los efectos respiratorios depresores y sedantes de la interación fármaco-fármaco (DDI) de la administración conjunta de GHB y etanol, y redujo la concentración cerebral y la relación de concentración cerebro-plasma de GHB[7].
References:
[1] Guan X, Rodriguez-Cruz V, Morris M E. Cellular uptake of MCT1 inhibitors AR-C155858 and AZD3965 and their effects on MCT-mediated transport of L-lactate in murine 4T1 breast tumor cancer cells[J]. The AAPS journal, 2019, 21: 1-10.
[2] Wang Z H, Peng W B, Zhang P, et al. Lactate in the tumour microenvironment: From immune modulation to therapy[J]. EBioMedicine, 2021, 73.
[3] Wang H, Zhou F, Qin W, et al. Metabolic regulation of myeloid-derived suppressor cells in tumor immune microenvironment: targets and therapeutic strategies[J]. Theranostics, 2025, 15(6): 2159.
[4] Ovens M J, Davies A J, Wilson M C, 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[J]. Biochemical Journal, 2010, 425(3): 523-530.
[5] Choi M C, Kim S K, Choi Y J, et al. Role of monocarboxylate transporter I/lactate dehydrogenase B-mediated lactate recycling in tamoxifen-resistant breast cancer cells[J]. Archives of Pharmacal Research, 2023, 46(11): 907-923.
[6] Guan X, Bryniarski M A, Morris M E. In vitro and in vivo efficacy of the monocarboxylate transporter 1 inhibitor AR-C155858 in the murine 4T1 breast cancer tumor model[J]. The AAPS journal, 2018, 21(1): 3.
[7] Rodriguez-Cruz V, Morris M E. γ-Hydroxybutyric Acid–Ethanol Drug-Drug Interaction: Reversal of Toxicity with Monocarboxylate Transporter 1 Inhibitors[J]. The Journal of Pharmacology and Experimental Therapeutics, 2021, 378(1): 42-50.
| Experimentos celulares [1]: | |
Líneas celulares | Células 4T1 |
Método de preparación | Las celdas 4T1 se chaparon en placas de 96 pozos a una densidad celular de 5,0×103 células por pozo en 100 μL de medio completo y se permitió adherirse durante la noche. El día del estudio, se retiró el medio y se lavó las células con PBS. Las células se trataron con 0-500nM AR-C155858 en 100 μL de medio libre de suero durante 48h. El crecimiento celular relativo se cuantificó utilizando el reactivo de proliferación celular WST-1. Los resultados se normalizaron al control del vehículo (< 0,1 % DMSO) y se expresaron como porcentaje de crecimiento celular. |
Condiciones de reacción | 0-500nM; 48h |
Áreas de aplicación | AR-C155858 exhibió un efecto inhibidor dependiente de la concentración sobre el crecimiento celular con un valor de IC50 de 20,3 nM. |
References: | |
| Cas No. | 496791-37-8 | SDF | |
| Chemical Name | 6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4S)-4-hydroxy-1,2-oxazolidine-2-carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione | ||
| Canonical SMILES | CC1=C(C(=NN1)C)CC2=C(C3=C(S2)N(C(=O)N(C3=O)C)CC(C)C)C(=O)N4CC(CO4)O | ||
| Formula | C21H27N5O5S | M.Wt | 461.53 |
| Solubility | DMSO: 100 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1667 mL | 10.8335 mL | 21.6671 mL |
| 5 mM | 433.3 μL | 2.1667 mL | 4.3334 mL |
| 10 mM | 216.7 μL | 1.0834 mL | 2.1667 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solution in DMSO
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)