Biological Activity
RGX-202 is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of cancer[1].
In Vitro
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[1].
In Vivo
RGX-202 (800 mg/kg; p.o. for 35 days) reduces UN-KPC-961 pancreatic tumoral creatine levels in B6129SF1/J mice[1]. RGX-202 (approximately 650 mg/kg; i.p. daily for 14 days) treatment reduces Lvm3b cells liver metastatic colonization by eightfold in NOD-SCID mice[1]. Animal Model: UN-KPC-961 pancreatic tumor-bearing B6129SF1/J mice[1] 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[1] 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.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.