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25mg |
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Purity: ≥98%
AR-C155858 is a novel, selective and potent inhibitor of monocarboxylate transporters MCT1 and MCT2 with Kis of 2.3 nM and 10 nM, respectively. It binds to an intracellular site involving transmembrane helices 7-10. Inhibitor titrations of L-lactate transport by MCT1 in rat erythrocytes were used to determine the Ki and number of AR-C155858-binding sites (Et) on MCT1 and the turnover number of the transporter (kcat). Derived values were 2.3+/-1.4 nM, 1.29+/-0.09 nmol per ml of packed cells and 12.2+/-1.1 s-1 respectively.
ln Vitro |
The MCT1/MCT2 C-terminal chimera is inhibited by AR-C155858 (10 nM–100 nM) [1]. MCT2 is inhibited by AR-C155858, with a 70% inhibition at 10 nM and a progressive increase in inhibition that is only consistent with Ki values much below 10 nM. In Xenopus laevis oocytes, AR-C155858 suppresses MCT1 expression in a concentration- and time-dependent manner[2].
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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 |
Molecular Formula |
C21H27N5O5S
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Molecular Weight |
461.5346
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CAS # |
496791-37-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1N(CC(C)C)C2=C(C(C(N3OC[C@@H](O)C3)=O)=C(CC4=C(C)NN=C4C)S2)C(N1C)=O
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InChi Key |
ISIVOJWVBJIOFM-ZDUSSCGKSA-N
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InChi Code |
InChI=1S/C21H27N5O5S/c1-10(2)7-25-20-17(18(28)24(5)21(25)30)16(19(29)26-8-13(27)9-31-26)15(32-20)6-14-11(3)22-23-12(14)4/h10,13,27H,6-9H2,1-5H3,(H,22,23)/t13-/m0/s1
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Chemical Name |
(S)-6-((3,5-dimethyl-1H-pyrazol-4-yl)methyl)-5-(4-hydroxyisoxazolidine-2-carbonyl)-1-isobutyl-3-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
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Synonyms |
ARC155858 AR-C155858 ARC 155858.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~70 mg/mL (~151.67 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.