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| Targets |
β-Glucuronidase. D-Saccharic acid 1,4-lactone hydrate is a potent and specific inhibitor of β-glucuronidase, a lysosomal enzyme that hydrolyzes glucuronides. By inhibiting this enzyme, DSAL prevents the hydrolysis of glucuronide conjugates, thereby affecting the enterohepatic circulation of drugs and endogenous compounds. It also potentially inhibits Klotho deglycosylation of excitatory amino acid transporters (EAATs) and peptide transporters (PEPTs).
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| ln Vitro |
In vitro, D-Saccharic acid 1,4-lactone hydrate is a potent inhibitor of β-glucuronidase, with an IC50 of 48.4 μM. It is used as a standard inhibitor in enzyme assays to study β-glucuronidase activity and to validate the specificity of the assay. Its activity is measured by its ability to inhibit the hydrolysis of a fluorogenic or chromogenic substrate, such as 4-methylumbelliferyl-β-D-glucuronide (4-MUG).
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| ln Vivo |
In vivo, D-Saccharic acid 1,4-lactone hydrate is used as a research tool to study the role of β-glucuronidase in various physiological and pathological processes. By inhibiting this enzyme, it can modulate drug metabolism and the enterohepatic circulation of compounds. It has also been studied for its potential anticarcinogenic and detoxifying effects in animal models.
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| Enzyme Assay |
The inhibitory activity of D-Saccharic acid 1,4-lactone hydrate on β-glucuronidase is measured in a cell-free enzyme assay. Purified β-glucuronidase is incubated with a fluorogenic substrate, such as 4-methylumbelliferyl-β-D-glucuronide (4-MUG), in the presence of varying concentrations of the inhibitor. The fluorescence generated by the hydrolysis of the substrate is measured, and the IC50 is calculated.
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| Cell Assay |
To study its effects on cellular metabolism, cells are treated with D-Saccharic acid 1,4-lactone hydrate. The activity of β-glucuronidase in cell lysates can be measured to confirm target inhibition. The effect on the metabolism of glucuronidated compounds can be assessed.
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| Animal Protocol |
The in vivo effects of D-Saccharic acid 1,4-lactone hydrate can be studied in animal models. The compound is administered orally or intraperitoneally. Its effect on the pharmacokinetics of drugs that undergo glucuronidation or on the levels of endogenous glucuronides can be assessed.
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| ADME/Pharmacokinetics |
D-Saccharic acid 1,4-lactone hydrate has a molecular weight of 210.14 g/mol and a molecular formula of C6H10O8. It is a solid that is soluble in water, DMSO, and methanol. It is typically stored at 2-8°C.
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| Toxicity/Toxicokinetics |
Specific toxicological data for D-Saccharic acid 1,4-lactone hydrate are not detailed, as it is a research compound. It is not intended for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Taha M, et al. Synthesis, β-glucuronidase inhibition and molecular docking studies of hybrid bisindole-thiosemicarbazides analogs. Bioorg Chem. 2016;68:56-63.
[2]. Bhattacharya S, et al. Prophylactic role of D-Saccharic acid-1,4-lactone in tertiary butyl hydroperoxide induced cytotoxicity and cell death of murine hepatocytes via mitochondria-dependent pathways. J Biochem Mol Toxicol. 2011;25(6):341-354. |
| Additional Infomation |
D-Saccharic acid 1,4-lactone hydrate is a valuable research tool for studying glucuronidation, detoxification, and the role of β-glucuronidase in drug metabolism and disease. Its ability to inhibit β-glucuronidase with high potency makes it a key reagent for investigating the enterohepatic circulation of drugs and endogenous compounds. It is also of interest for its potential health benefits, including anticarcinogenic and antioxidant effects. It is not a drug and is not approved for therapeutic use.
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| Molecular Formula |
C6H10O8
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| Molecular Weight |
210.14
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| Exact Mass |
192.027
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| CAS # |
61278-30-6
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| PubChem CID |
20055579
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| Appearance |
White to off-white solid powder
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| Melting Point |
80-82ºC
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
237
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| Defined Atom Stereocenter Count |
4
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| SMILES |
[C@H]1([C@H](C(=O)O[C@@H]1[C@@H](C(=O)O)O)O)O.O
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| InChi Key |
NPFKVZHSFSFLPU-QGBSHYGGSA-N
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| InChi Code |
InChI=1S/C6H8O7.H2O/c7-1-2(8)6(12)13-4(1)3(9)5(10)11;/h1-4,7-9H,(H,10,11);1H2/t1-,2-,3+,4+;/m1./s1
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| Chemical Name |
(2S)-2-[(2S,3R,4R)-3,4-dihydroxy-5-oxooxolan-2-yl]-2-hydroxyacetic acid;hydrate
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| 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)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (1189.68 mM)
H2O: ≥ 100 mg/mL (475.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (9.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (9.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7587 mL | 23.7937 mL | 47.5873 mL | |
| 5 mM | 0.9517 mL | 4.7587 mL | 9.5175 mL | |
| 10 mM | 0.4759 mL | 2.3794 mL | 4.7587 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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