RGX-202

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RGX-202  纯度: ≥95.0%

RGX-202 是一种具有口服活性的 SLC6A8 转运蛋白抑制剂。RGX-202 在体外和体内均强烈抑制肌酸输入，降低细胞内磷酸肌酸和 ATP 水平，并诱导肿瘤凋亡 (apoptosis)。RGX-202 可用于肿瘤的研究。

RGX-202

RGX-202 Chemical Structure

CAS No. : 353-09-3

规格 价格 是否有货 数量
50 mg ￥350 In-stock
100 mg ￥520 In-stock
200 mg   询价  
500 mg   询价  

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RGX-202 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Human Endogenous Metabolite Compound Library
  • Orally Active Compound Library
  • Rare Diseases Drug Library

生物活性

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].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

131.14

Formula

C4H9N3O2
CAS 号

353-09-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Kurth I, et al. Therapeutic targeting of SLC6A8 creatine transporter suppresses colon cancer progression and modulates human creatine levels. Sci Adv. 2021 Oct 8;7(41):eabi7511.

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