| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
- Fosfructose trisodium is an endogenous metabolite that acts as an allosteric activator of several enzymes in glycolysis, including:
- Phosphofructokinase-1 (PFK-1): critical rate-limiting enzyme in glycolysis [1] - Pyruvate kinase: converts phosphoenolpyruvate to pyruvate [1] - NAD⁺-dependent L-(+)-lactate dehydrogenase: involved in anaerobic energy production [1] - It also acts as an inhibitor of acetate kinase and serves as a substrate for fructose-1,6-bisphosphate aldolase and fructose-1,6-bisphosphatase [1] |
|---|---|
| ln Vitro |
- In cellular assays, Fosfructose trisodium (500 μg/ml) significantly increased tissue levels of FDP (0.22 ± 0.01 mg/g) compared to control (0.14 ± 0.004 mg/g, p=0.0006) [1]
- It stimulates anaerobic glycolysis, increasing ATP production under ischemic conditions [1] - As an allosteric regulator, it enhances glucose utilization and energy metabolism in cells [1] |
| ln Vivo |
- In a carrageenan-induced rat paw edema model, Fosfructose trisodium showed anti-inflammatory effects by reducing edema formation through enhanced energy supply to ischemic tissues [1]
- In sickle cell anemia models, it improved red blood cell flexibility and reduced vaso-occlusive crises by increasing intracellular ATP levels [1] - In cardiovascular ischemia models, it protected cardiac function by preserving ATP levels during hypoxia and enhancing post-ischemic recovery [1] |
| ADME/Pharmacokinetics |
In healthy volunteers, intravenous injection of trisodium fructose phosphate (250 mg/kg) resulted in a plasma concentration of 770 mg/L within 5 minutes, with a half-life of 10-15 minutes [1]. It rapidly distributes to extravascular tissues and is hydrolyzed into inorganic phosphate and fructose, which are subsequently metabolized or excreted [1]. In rats, trisodium fructose phosphate levels in blood and brain tissue increased synchronously without delay, but levels in liver, kidney, muscle, and fat returned to baseline levels within 12 hours, while levels in blood and brain tissue remained elevated [1]. Due to hydrolysis and first-pass metabolism in the gastrointestinal tract, its oral bioavailability is low [1].
|
| Toxicity/Toxicokinetics |
Acute toxicity in mice and rabbits: The lethal doses at infusion rates of 0.4–0.6 g/kg/min were 5.0 g/kg and 5.8 g/kg, respectively [1]
- The toxicity appears to be related to the large amount of inorganic phosphate entering the bloodstream after high-dose hydrolysis [1] - Adverse clinical reactions included flushing, palpitations, and numbness in the hands and feet when the infusion rate exceeded 10 ml/min [1] - Rare reports of allergic reactions and anaphylactic shock [1] |
| References | |
| Additional Infomation |
See also: Fructose trisodium phosphate (note moved to).
- Fructose trisodium phosphate (also known as fructose trisodium diphosphate or esafofen trisodium) is a cell-protective natural sugar phosphate developed by Questcor Pharmaceuticals for the treatment of cardiovascular ischemia, sickle cell anemia and asthma[1] - It has been granted orphan drug designation for the treatment of vascular occlusive crisis in sickle cell anemia[1] - Mechanism of action: Enhances energy production in ischemic tissues by stimulating anaerobic glycolysis, increasing ATP and creatine phosphate concentrations, promoting potassium influx, increasing erythrocyte 2,3-diphosphoglycerate levels, and inhibiting oxygen free radical and histamine release[1] - It is the trisodium salt of fructose D-1,6-diphosphate with the molecular formula C₆H₁₁Na₃O₁₂P₂ and a molecular weight of 406.06 g/mol[1] |
| Molecular Formula |
C6H11NA3O12P2
|
|---|---|
| Molecular Weight |
406.0612
|
| Exact Mass |
405.941
|
| CAS # |
38099-82-0
|
| Related CAS # |
Fosfructose;488-69-7
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| PubChem CID |
90264
|
| Appearance |
White to off-white solid powder
|
| Density |
2.095g/cm3
|
| Boiling Point |
722.6ºC at 760mmHg
|
| Melting Point |
127ºC
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| Flash Point |
390.8ºC
|
| LogP |
-5.6
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
24
|
| Complexity |
387
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
P(=O)([O-])([O-])OC([H])([H])[C@]([H])([C@]([H])([C@@]([H])(C(C([H])([H])OP(=O)([O-])O[H])=O)O[H])O[H])O[H].[Na+].[Na+].[Na+]
|
| InChi Key |
RNBGYGVWRKECFJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C6H14O12P2/c7-4-3(1-16-19(10,11)12)18-6(9,5(4)8)2-17-20(13,14)15/h3-5,7-9H,1-2H2,(H2,10,11,12)(H2,13,14,15)
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| Chemical Name |
[2,3,4-trihydroxy-5-(phosphonooxymethyl)oxolan-2-yl]methyl dihydrogen phosphate
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~150 mg/mL (~369.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (246.27 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4627 mL | 12.3135 mL | 24.6269 mL | |
| 5 mM | 0.4925 mL | 2.4627 mL | 4.9254 mL | |
| 10 mM | 0.2463 mL | 1.2313 mL | 2.4627 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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