3-Guanidinopropionic Acid (Synonyms: β-GPA,PNU 10483) |
| Catalog No.GC13992 |
RGX-202 (3-Guanidinopropionic acid) 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 and duchenne muscular dystrophy.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 353-09-3
Sample solution is provided at 25 µL, 10mM.
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3-Guanidinopropionic Acid is an AMP-activated protein kinase (AMPK) stimulator and PPARγ coactivator 1α (PGC-1α) activator.
AMP-activated protein kinase is an enzyme involved in cellular energy homeostasis. AMPK activation has been involved in stimulation of hepatic fatty acid oxidation, ketogenesis, skeletal muscle fatty acid oxidation and glucose uptake, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, and modulation of insulin secretion by pancreatic beta-cells [1]. PGC-1α is a transcriptional coactivator involved in regulating the genes implicated in energy metabolism and mitochondrial biogenesis, such as the the expression of AMPK, genes for oxidative phosphorylation, electron transport chain, and mitochondrial biogenesis, increasing oxidative muscle fibers, numbers of mitochondria, and motor performance [2].
3-Guanidinopropionic acid improved insulin sensitivity and promoted weight loss selectively from adipose tissue in animal models of non-insulin-dependent diabetes mellitus (NIDDM). 3-Guanidinopropionic acid was a substrate for both the creatine transporter and creatine kinase [3]. In KKAy mice with noninsulin-dependent diabetes, 3-guanidinopropionic acid decreased the plasma glucose level. In insulin-resistant rhesus monkeys, 3-guanidinopropionic acid increased the disappearance of i.v. glucose [4].
References:
[1] Winder W W, Hardie D G. AMP-activated protein kinase, a metabolic master switch: possible roles in type 2 diabetes[J]. American Journal of Physiology-Endocrinology And Metabolism, 1999, 277(1): E1-E10.
[2] Chaturvedi, R. K.,Adhihetty, P.,Shukla, S., et al. Impaired PGC-1α function in muscle in Huntington’s disease. Human Molecular Genetics 18(16), 3048-3065 (2009).
[3] Larsen S D, Connell M A, Cudahy M M, et al. Synthesis and biological activity of analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid: discovery of a novel aminoguanidinoacetic acid antidiabetic agent[J]. Journal of medicinal chemistry, 2001, 44(8): 1217-1230.
[4] Meglasson M D, Wilson J M, Yu J H, et al. Antihyperglycemic action of guanidinoalkanoic acids: 3-guanidinopropionic acid ameliorates hyperglycemia in diabetic KKAy and C57BL6Job/ob mice and increases glucose disappearance in rhesus monkeys[J]. Journal of Pharmacology and Experimental Therapeutics, 1993, 266(3): 1454-1462.
| Cas No. | 353-09-3 | SDF | |
| Synonyms | β-GPA,PNU 10483 | ||
| Chemical Name | N-(aminoiminomethyl)-β-alanine | ||
| Canonical SMILES | NC(NCCC(O)=O)=N | ||
| Formula | C4H9N3O2 | M.Wt | 131.1 |
| Solubility | ≥ 13.1mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 7.6278 mL | 38.1388 mL | 76.2777 mL |
| 5 mM | 1.5256 mL | 7.6278 mL | 15.2555 mL |
| 10 mM | 0.7628 mL | 3.8139 mL | 7.6278 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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