| Size | Price | |
|---|---|---|
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Isoascorbic acid is readily absorbed and metabolized. In human subjects, oral administration of 500 mg of isoascorbic acid resulted in similar upward trends in the concentration curves of both ascorbic acid and isoascorbic acid in the blood. In five human subjects, oral administration of 300 mg of isoascorbic acid had no effect on the excretion of ascorbic acid in urine. In hamsters, rats, and rabbits, L-ascorbic acid is poorly absorbed in the intestines due to its non-essential nature, primarily through passive diffusion; conversely, in guinea pigs and humans, ascorbic acid absorption is mediated by a saturable, sodium-dependent active transport mechanism. Therefore, the first few animal groups are unsuitable as models for human absorption. Because the active transport system is saturable, but passive diffusion can also play a significant role at high dose levels, ascorbic acid absorption is dose-dependent. Isoascorbic acid appears to be another substrate in the same transport system, but its activity is much lower than that of L-ascorbic acid, thus it may act as a weak competitive inhibitor of L-ascorbic acid absorption. In studies using brush border vesicles isolated from guinea pig ileum, K1 values were estimated to be approximately 11 mM and 20 mM; in contrast, the apparent Km value for ascorbic acid absorption in the same system was approximately 0.3 mM. The lack of stronger antiscurvy activity of isoascorbic acid may be due to the fact that tissues cannot retain it as efficiently as they do for storing ascorbic acid. Absorption of isoascorbic acid via the human buccal mucosa was investigated in healthy adult subjects. The absorption of a 10 mM isoascorbic acid solution at pH 6 was 13.0 ± 0.74 μmol/5 min. No statistically significant difference was found in the absorption of isoascorbic acid and L-ascorbic acid. For more complete data on the absorption, distribution, and excretion of isoascorbic acid (13 items in total), please visit the HSDB record page. Biological half-life In dogs, this results in a plasma half-life of approximately 30 minutes for isoascorbic acid. |
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| Toxicity/Toxicokinetics |
Interactions
This study investigated the regulatory effects of three antioxidants—sodium L-ascorbate (SA), ascorbic acid (AA), and sodium isoascorbate (SE)—on the two-stage development of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced gastric cancer in F344 rats. Dietary supplementation with 5% SE significantly reduced the incidence of pyloric dysplasia and had a minor effect on the incidence of forestomach papillomas; however, no such effects were observed with the addition of 5% and 1% SA, or 5% AA. These results suggest that SE has a weak inhibitory effect on gastric cancer development. Sodium isoascorbate: Rapid intravenous administration of tetracycline hydrochloride (50 mg/kg) resulted in significant azotemia and other signs of kidney damage in rats and dogs, which were prevented by concurrent administration of ascorbic acid (125 mg/kg or higher). D-isoascorbic acid showed similar effects in rat studies. Non-human toxicity values Oral LD50 in mice: 8.3 g/kg Oral LD50 in rats: 18.0 g/kg |
| Additional Infomation |
D-Isoascorbic acid is an ascorbic acid. It has been reported to be found in Hypsizygus marmoreus, Grifola frondosa, and other organisms with relevant data. Therapeutic Uses: Isoascorbic acid is a stereoisomer of L-ascorbic acid and is used as an antioxidant in food and oral pharmaceutical preparations. Its vitamin C activity is approximately 5% that of L-ascorbic acid.
|
| Molecular Formula |
C6H8O6
|
|---|---|
| Molecular Weight |
176.1241
|
| Exact Mass |
176.032
|
| CAS # |
89-65-6
|
| Related CAS # |
Sodium erythorbate;6381-77-7
|
| PubChem CID |
54675810
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
2.0±0.1 g/cm3
|
| Boiling Point |
552.7±50.0 °C at 760 mmHg
|
| Melting Point |
167-172ºC
|
| Flash Point |
238.2±23.6 °C
|
| Vapour Pressure |
0.0±3.4 mmHg at 25°C
|
| Index of Refraction |
1.711
|
| LogP |
-2.41
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
12
|
| Complexity |
232
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C([C@H]([C@@H]1C(=C(C(=O)O1)O)O)O)O
|
| InChi Key |
CIWBSHSKHKDKBQ-DUZGATOHSA-N
|
| InChi Code |
InChI=1S/C6H8O6/c7-1-2(8)5-3(9)4(10)6(11)12-5/h2,5,7-10H,1H2/t2-,5-/m1/s1
|
| Chemical Name |
(2R)-2-[(1R)-1,2-dihydroxyethyl]-3,4-dihydroxy-2H-furan-5-one
|
| 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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
DMSO : ~125 mg/mL (~709.74 mM)
H2O : ~83.33 mg/mL (~473.14 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (567.79 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 | 5.6779 mL | 28.3897 mL | 56.7795 mL | |
| 5 mM | 1.1356 mL | 5.6779 mL | 11.3559 mL | |
| 10 mM | 0.5678 mL | 2.8390 mL | 5.6779 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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