1. Apoptosis Metabolic Enzyme/Protease
  2. Apoptosis Endogenous Metabolite
  3. Ompenaclid

Ompenaclid  (Synonyms: RGX-202; 3-Guanidinopropionic acid)

Cat. No.: HY-W015828 Purity: 99.94%
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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.

For research use only. We do not sell to patients.

CAS No. : 353-09-3

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Ompenaclid:

Top Publications Citing Use of Products

    Ompenaclid purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2489072.  [Abstract]

    Ompenaclid (RGX-202: 800 mg/kg). Protein bands of AMPKα, p-AMPKα, ACC, p-ACC, ACSL4 and COX2 in mouse ileum.

    Ompenaclid purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2489072.  [Abstract]

    TUNEL staining shows the effect of RGX-202 (Ompenaclid: 800 mg/kg) administration on DTRF radioprotection. Dead cells are shown as green fluorescence. Cell nuclei are stained with DAPI (blue).

    Ompenaclid purchased from MedChemExpress. Usage Cited in: Res Sq. 2024 Aug 06.

    HE staining revealing the impact of RGX-202 (Ompenaclid:800 mg/kg) administration on the radioprotection of DTRF.

    Ompenaclid purchased from MedChemExpress. Usage Cited in: Oncoimmunology. 2023 Apr 19;12(1):2204015.

    Intracellular and extracellular levels of creatine in WT BMDCs treated with PBS or Ompenaclid (RGX202).

    Ompenaclid purchased from MedChemExpress. Usage Cited in: Oncoimmunology. 2023 Apr 19;12(1):2204015.

    Ompenaclid (RGX202). CD8 levels in T cells and IFN-γ levels in CD8+ T cells co-cultured with BMDCs.

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    • Biological Activity

    • Purity & Documentation

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    Description

    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[1][2].

    IC50 & Target

    Human Endogenous Metabolite

     

    In Vitro

    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[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Ompenaclid (RGX-202; 800 mg/kg; p.o. for 35 days) reduces UN-KPC-961 pancreatic tumoral creatine levels in B6129SF1/J mice[1].
    Ompenaclid (approximately 650 mg/kg; i.p. daily for 14 days) treatment reduces Lvm3b cells liver metastatic colonization by eightfold in NOD-SCID mice[1].

    MedChemExpress (MCE) 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.
    Clinical Trial
    Molecular Weight

    131.14

    Formula

    C4H9N3O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CCNC(N)=N

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 50 mg/mL (381.27 mM)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 7.6254 mL 38.1272 mL 76.2544 mL
    5 mM 1.5251 mL 7.6254 mL 15.2509 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.94%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 7.6254 mL 38.1272 mL 76.2544 mL 190.6360 mL
    5 mM 1.5251 mL 7.6254 mL 15.2509 mL 38.1272 mL
    10 mM 0.7625 mL 3.8127 mL 7.6254 mL 19.0636 mL
    15 mM 0.5084 mL 2.5418 mL 5.0836 mL 12.7091 mL
    20 mM 0.3813 mL 1.9064 mL 3.8127 mL 9.5318 mL
    25 mM 0.3050 mL 1.5251 mL 3.0502 mL 7.6254 mL
    30 mM 0.2542 mL 1.2709 mL 2.5418 mL 6.3545 mL
    40 mM 0.1906 mL 0.9532 mL 1.9064 mL 4.7659 mL
    50 mM 0.1525 mL 0.7625 mL 1.5251 mL 3.8127 mL
    60 mM 0.1271 mL 0.6355 mL 1.2709 mL 3.1773 mL
    80 mM 0.0953 mL 0.4766 mL 0.9532 mL 2.3829 mL
    100 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9064 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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