5.33436

Monocarboxylate Transport Inhibitor, AR-C155858

• 동의어(들): Monocarboxylate Transport Inhibitor, AR-C155858, (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 , Monocarboxylate transporter 1 inhibitor, AR-C155858, SR13801
• 실험식(Hill 표기법): C₂₁H₂₇N₅O₅S
• CAS Number: 496791-37-8
• Molecular Weight: 461.53
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥95% (HPLC)
• Quality Level: 100
• 형태: solid
• 효능: 1.2 nM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: brown
• solubility: DMSO: 50 mg/mL
• 저장 온도: −20°C
• 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
• InChI key: ISIVOJWVBJIOFM-ZDUSSCGKSA-N

설명

일반 설명

A cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i = 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC₅₀ = 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.

A cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i = 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC₅₀ = 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Monocarboxylate Transport Inhibitor, AR-C155858, CAS 496791-37-8, is a cell-permeable, potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i = 2.3 nM for lactate uptake in rat erythrocytes).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
MCT1

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Nancolas, B., et al. 2015. Biochem. J.467, 192.
Ovens, M. J. et al. 2010. Biochem. J.425, 523.
Guile, S. D., et al. 2007. J. Med. Chem.50, 254.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable