AR-C155858
496791-37-8
0.98%
2026-10-19
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName AR-C155858 Cat No CEI-1216 Product Overview AR-C155858 is a potent and selective inhibitor of monocarboxylate transporters MCT1 and MCT2 with Ki values of 2.3nM and less than 10 nM, respectively. MCT is a monocarboxylate transporter family with 14 members. Among these transporters, MCT1 and MCT2 are worked for the uptake and efflux of lactic acid. As a selective inhibitor of MCT1 and MCT2, AR-C155858 can be used to probe MCTs'roles in the metabolic studies. Besides that, AR-C155858 was found to have immunosuppressive activity and can inhibit the proliferation of T-lymphocytes. The binding site of MCT1 for AR-C155858 contains transmembrane helices 7-10 in C-terminal domain. The two residues Phe360 and Ser364 play important roles in the binding. In rat erythrocytes in which the AE1 mediated lactate transport had been blocked, AR-C155858 inhibited endogenous MCT1 mediated L-lactate uptake dose-dependently. AR-C155858 showed to be a tight-binding non-competitive inhibitor with Ki value of 2.3±1.4 nM and Kcat value of 12.2±1.1 s-1.In Xenopus oocytes expressing MCT1, MCT2 or MCT4, AR-C155858 at concentration of 100 nM showed 100% inhibition of MCT1 mediated lactate uptake. For MCT2, AR-C155858 at 10 nM showed 70% inhibition. AR-C155858 had no significant effect against MCT4 even at concentration up to 10 μM. In addition, it has been found that the inhibition of MCTs caused by AR-C155858 can be affected by the co-expression of ancillary proteins. The presence of embigin reduced the sensitivity of MCT2 against AR-C155858's inhibition. AR-C155858 potently suppressed the uptake of lactic acid in Ras-transformed fibroblast CCL39 cells via inhibiting MCT1 and MCT2 but no MCT4.The suppression subsequently resulted in significant decrease of glycolysis. In nude mice implanted with Ras-transformed CCL39 fibroblasts, the administration of AR-C155858 at dose of 30 mg/kg twice daily resulted in significant tumor growth suppression CAS No 496791-37-8 Molecular Weight 461.53 Purity 0.98 Storage Store at -20°C Synonyms AR C155858 Targets MCT1; MCT2 Molecular Formula C21H27N5O5S 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 Solubility Soluble in DMSO > 10 mM Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Specialty Chemicals(c26) cas_num 496791-37-8 Basic Info-
Product Name:
(S)-6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4-hydroxyisoxazolidin-2-yl)carbonyl]-1-isobutyl-3-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Other Name:6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;(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;(S)-6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4-hydroxyisoxazolidin-2-yl)carbonyl]-1-isobutyl-3-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;AR C15585;AR-C 155858;AR C15585;AR-C155858;AR C155858;AR-C 155858;Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)-
CAS No.:496791-37-8
Molecular Formula:C21H27N5O5S
InChIKeys:ISIVOJWVBJIOFM-ZDUSSCGKSA-N
Molecular Weight:461.53
Exact Mass:461.17329015
DSSTox ID:DTXSID70436993
Categories:
Characteristics-
PSA:
150.69000
XLogP3:1.03460
Density:1.395
Melting Point:198-202∶C
Boiling Point:763.1±70.0 °C(Predicted)
PKA:13.53±0.20
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15 days
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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Country Product Purchase Quantity Date Posted Post an enquiry for this product
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