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编 号:F333174
分子式:C4H9N3O2
分子量:131.14
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50mg
280
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100mg
416
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生物活性:
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy.

体内研究:
Ompenaclid (RGX-202; 800 mg/kg; p.o. for 35 days) reduces UN-KPC-961 pancreatic tumoral creatine levels in B6129SF1/J mice.?Ompenaclid (approximately 650 mg/kg; i.p. daily for 14 days) treatment reduces Lvm3b cells liver metastatic colonization by eightfold in NOD-SCID mice.Animal Model:UN-KPC-961 pancreatic tumor-bearing B6129SF1/J mice
Dosage:800 mg/kg
Administration:p.o. for 35 days
Result:Suppressed tumoral d3-creatine import by 50% at 800 mg/kg.
Animal Model:6- to 9-week-old C57BL/6J male wild-type mice
Dosage:100, 250, 500 mg/KG in sterile 0.9% NaCl
Administration:p.o. for 35 days
Result:Inhibited tissue uptake of d3-creatine in a dose-dependent manner by up to 75% at 500 mg/kg.

体外研究:
Ompenaclid (RGX-202; 10 μM; 96 hours) reduces cell growth, and reveals a nearly complete depletion of phosphocreatine (>99%), greater than 79% reduction in cellular creatine and a substantial (46%) reduction in intracellular ATP levels relative to control cells in hypoxia.
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