Ompenaclid
Based on 6 publication(s) in Google Scholar
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.
- Purity : 99.94%
- CAS No.: 353-09-3
- Formula: C4H9N3O2
- Molecular Weight:131.14
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-W010388
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Publications Citing Use of MedChemExpress (MCE) Ompenaclid
More- Gut Microbes. 2025 Dec;17(1):2489072. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Sep 9;122(36):e2426135122. [Abstract]
- Cancer Immunol Res. 2025 Jun 4;13(6):939-956. [Abstract]
- Oncoimmunology. 2023 Apr 19;12(1):2204015. [Abstract]
- ACS Omega. 2025 Aug 21;10(34):39192-39202. [Abstract]
- Res Sq. 2024 Aug 06.
Customer Validation & Images
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WB
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Histological Imaging/Staining
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Histological Imaging/Staining
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Others
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Flow Cytometry
All Endogenous Metabolite Isoforms
More
Biological Activity
Description
IC50 & Target
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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. Further protocols information, click here.
In Vivo
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.
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Animal Model:UN-KPC-961 pancreatic tumor-bearing B6129SF1/J mice[1]
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Dosage:800 mg/kg
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Administration:p.o. for 35 days
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Result:Suppressed tumoral d3-creatine import by 50% at 800 mg/kg.
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Animal Model:6- to 9-week-old C57BL/6J male wild-type mice[1]
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Dosage:100, 250, 500 mg/KG in sterile 0.9% NaCl
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Administration:p.o. for 35 days
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Result:Inhibited tissue uptake of d3-creatine in a dose-dependent manner by up to 75% at 500 mg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 353-09-3
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Appearance Solid
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Molecular Weight 131.14
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Formula C4H9N3O2
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Color White to off-white
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SMILES
O=C(O)CCNC(N)=N
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Synonyms
RGX-202; 3-Guanidinopropionic acid
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Gut Microbes
Creatine-mediated ferroptosis inhibition is involved in the intestinal radioprotection of daytime-restricted feeding. [Abstract]2025 Dec;17(1):2489072. PMID: 40205678
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).
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Proc Natl Acad Sci U S A
Structural insights into the substrate uptake and inhibition of the human creatine transporter (hCRT). [Abstract]2025 Sep 9;122(36):e2426135122. PMID: 40892912 -
Cancer Immunol Res
In Situ Delivery of Gasdermin E mRNA Promotes Antitumor Immunity via Creatine-Elicited Type I Interferon Signaling in Monocytes. [Abstract]2025 Jun 4;13(6):939-956. PMID: 40168141 -
Oncoimmunology
CARD9 deficiency promotes pancreatic cancer growth by blocking dendritic cell maturation via SLC6A8-mediated creatine transport. [Abstract]2023 Apr 19;12(1):2204015. PMID: 37089447
Ompenaclid purchased from MedChemExpress. Usage Cited in: Oncoimmunology. 2023 Apr 19;12(1):2204015. [Abstract]
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. [Abstract]
Ompenaclid (RGX202). CD8 levels in T cells and IFN-γ levels in CD8+ T cells co-cultured with BMDCs.
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ACS Omega
2025 Aug 21;10(34):39192-39202. PMID: 40918390 -
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.
Solvent & Solubility
In Vitro:
H2O : ≥ 50 mg/mL (381.27 mM)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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 |
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| 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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