| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
|
| Targets |
Human Endogenous Metabolite
|
|---|---|
| ln Vitro |
Ompenaclid (RGX-202; 10 μM; 96 hours) inhibits cell growth and shows almost total phosphocreatine depletion (>99%), cellular creatine reduction of over 79%, and a significant (46%) reduction in intracellular ATP levels in comparison to control cells under hypoxia[1].
|
| ln Vivo |
In B6129SF1/J mice, ommepenaclid (RGX-202; 800 mg/kg; po for 35 days) lowers the levels of UN-KPC-961 pancreatic tumoral creatine[1]. In NOD-SCID mice, omepenaclid (around 650 mg/kg; intraperitoneally every day for 14 days) inhibits treatment-induced liver metastatic colonization of Lvm3b cells by an eight-fold margin[1].
|
| Animal Protocol |
Animal/Disease Models: UN-KPC-961 pancreatic tumor-bearing B6129SF1/J mice[1]
Doses: 800 mg/kg Route of Administration: po for 35 days Experimental Results: Suppressed tumoral d3-creatine import by 50% at 800 mg/kg. Animal/Disease Models: 6- to 9weeks old C57BL/6J male wild- type mice[1] Doses: 100, 250, 500 mg/KG in sterile 0.9% NaCl Route of Administration: po for 35 days Experimental Results: Inhibited tissue uptake of d3-creatine in a dose-dependent manner by up to 75% at 500 mg/ kg. |
| References |
|
| Additional Infomation |
3-guanidinopropanoic acid is a guanidine compound bearing an N-(2-carboxyethyl) substituent. It is a creatine analogue that has been found to decreases plasma glucose levels It has a role as a hypoglycemic agent. It is functionally related to a propionic acid. It is a tautomer of a 3-guanidinopropanoic acid zwitterion.
RGX-202 is a recombinant AAV8 that contains a vector genome encoding a miniaturized dystrophin protein (microdystrophin). Ompenaclid is an orally available, small molecule inhibitor of the creatine transporter, solute carrier family 6, member 8 (SLC6a8), with potential antineoplastic activity. Upon oral administration, ompenaclid inhibits phosphocreatine uptake by SLC6a8, thereby reducing intracellular levels of phosphocreatine available for ATP synthesis in tumor cells. SLC6a8 is overexpressed in some cancer types and inhibition of its activity may potentially limit tumor cell growth and metastasis. |
| Molecular Formula |
C4H9N3O2
|
|---|---|
| Molecular Weight |
131.14
|
| Exact Mass |
131.069
|
| CAS # |
353-09-3
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| PubChem CID |
67701
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
299.1±42.0 °C at 760 mmHg
|
| Melting Point |
222 °C (dec.)(lit.)
|
| Flash Point |
134.7±27.9 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.575
|
| LogP |
-1.68
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
9
|
| Complexity |
128
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KMXXSJLYVJEBHI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C4H9N3O2/c5-4(6)7-2-1-3(8)9/h1-2H2,(H,8,9)(H4,5,6,7)
|
| Chemical Name |
3-(diaminomethylideneamino)propanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ≥ 50 mg/mL (381.27 mM)
DMSO : < 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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