[CAS NO. 353-09-3] Ompenaclid
PRODUCTS SPECIFICATIONS [353-09-3]
DESCRIPTION [353-09-3]
Overview
| MDL | MFCD00045939 |
|---|---|
| Molecular Weight | 131.14 |
| Molecular Formula | C4H9N3O2 |
| SMILES | O=C(O)CCNC(N)=N |
Summary
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] .
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]
.
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. |
Appearance
Solid
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
H 2 O : ≥ 50 mg/mL ( 381.27 mM )
DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)
* "≥" means soluble, but saturation unknown.
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 |
| 10 mM | 0.7625 mL | 3.8127 mL | 7.6254 mL |
References
- [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.
- [2] Creisméas A, et, al. TRPC1 and TRPC3 involvement in DMD physiopathology and as potential targets for treatment in complement to rAAV-microdystrophin. 2021 Oct 1;13.
Synonyms
