| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
FBPase-IN-1 targets fructose-1,6-bisphosphatase (FBPase), a key enzyme in the gluconeogenesis pathway that catalyzes the hydrolysis of fructose-1,6-bisphosphate to fructose-6-phosphate. FBPase is a rate-limiting enzyme in gluconeogenesis, and its inhibition reduces hepatic glucose production. The compound modifies the C128 site and regulates the N125-S124-S123 allosteric pathway of FBPase, affecting its catalytic activity. By inhibiting FBPase, the compound reduces blood glucose levels, making it a potential therapeutic for type 2 diabetes.
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| ln Vitro |
FBPase-IN-1 (compound 3a) has an IC50 of 75.08 μM and has minimal cytotoxicity (1.5625-200 μM, 48 hours) [1]. With an IC50 reduction from 0.28 μM to 0.09 μM, FBPase-IN-1 (0-45 minutes) inhibits FBPase in a time-dependent manner, suggesting that it is an irreversible covalent inhibitor of FBPase [1].
FBPase-IN-1 inhibits fructose-1,6-bisphosphatase with an IC50 of 0.22 μM. The compound is an irreversible inhibitor that modifies the C128 site of FBPase and regulates the N125-S124-S123 allosteric pathway, affecting catalytic activity. It reduces blood glucose levels and ameliorates glucose tolerance. The compound is used in studies of type 2 diabetes and gluconeogenesis. It functions as a herbicide in addition to its antidiabetic activity. |
| ln Vivo |
FBPase-IN-1 (12-hour starved ICR mice, n = 6 male, 25 mg/kg, IP) met the in vivo hypoglycemic effect (in vivo hypoglycemic impact Sugar effect is decreased by 54%) blood sugar is 25 mg/kg) and demonstrated good FBPase inhibitory activity (IC50 = 0.22 μM) [1]. By blocking the GNG process and targeting FBPase, FBPase-IN-1 (6 or 7 weeks, ICR mice, n = 6, male, 25 mg/kg, intraperitoneally administered once, 4 hours) lowers blood glucose levels [1].
In vivo, FBPase-IN-1 reduces blood glucose levels and ameliorates glucose tolerance in animal models. The compound has been studied for its potential in treating type 2 diabetes by inhibiting hepatic glucose production. By targeting FBPase, a rate-limiting enzyme in gluconeogenesis, the compound reduces the production of glucose from non-carbohydrate precursors. Specific dosing regimens and efficacy data would be determined from preclinical studies. |
| Enzyme Assay |
The in vitro enzyme assay for FBPase-IN-1 typically involves measuring the inhibition of FBPase activity. Recombinant FBPase enzyme is incubated with varying concentrations of FBPase-IN-1 (typically 0.001-100 μM) in the presence of the substrate fructose-1,6-bisphosphate. The enzymatic activity is measured by monitoring the production of fructose-6-phosphate or the release of inorganic phosphate using colorimetric or coupled enzyme assays. The IC50 value is determined by plotting the percentage of inhibition against compound concentration. The compound is dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
In vitro cellular assays for FBPase-IN-1 typically involve treating hepatocytes or other glucose-producing cells with the compound at concentrations ranging from 0.001 to 10 μM for 4-24 hours. Glucose production is measured by assaying the medium for glucose using glucose oxidase or other methods. Cell viability is assessed using MTT or other standard assays. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium. The compound's effects on gluconeogenesis are assessed by measuring the conversion of substrates to glucose.
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| Animal Protocol |
Animal/Disease Models: ICR mice (fasted for 12 hrs (hrs (hours)), n = 6, male) [1]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip) injection, once Experimental Results:Lower blood sugar. Animal/Disease Models: ICR mice (6 or 7 weeks, n = 6, male) [1] Doses: 25 mg/kg Route of Administration: IP for 4 hrs (hrs (hours)) once Experimental Results: Lowers blood glucose by targeting FBPase and inhibiting the GNG process level. In vivo animal studies for FBPase-IN-1 typically involve administering the compound to mice or rats via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Blood glucose levels are measured at various time points after administration. Glucose tolerance tests are performed to assess the compound's effects on glucose homeostasis. The compound's effects on hepatic glucose production are evaluated by measuring gluconeogenesis in liver tissue. The compound's pharmacokinetics and pharmacodynamics are assessed in these models. |
| ADME/Pharmacokinetics |
FBPase-IN-1 has a molecular weight of 232.37 g/mol and formula C6H4N2S4. The compound is chemically identified as 2,2'-dithiobis(thiazole). Recommended storage conditions are typically -20°C for powder and -80°C for solvent. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination. The compound's molecular weight and structural features suggest it may have moderate oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicity data for FBPase-IN-1 are not extensively reported. The compound is intended for research use only and is not approved for human therapeutic applications. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. As an FBPase inhibitor targeting gluconeogenesis, the compound may affect normal glucose homeostasis, which could contribute to potential toxicity. Appropriate safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
FBPase-IN-1 (CAS 20362-54-3) is a potent, irreversible inhibitor of fructose-1,6-bisphosphatase (FBPase) with an IC50 of 0.22 μM. It has a molecular weight of 232.37 g/mol and formula C6H4N2S4. The compound reduces blood glucose levels and ameliorates glucose tolerance. It is used in studies of type 2 diabetes and gluconeogenesis. The compound is chemically identified as 2,2'-dithiobis(thiazole). It is not approved for clinical use.
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| Molecular Formula |
C6H4N2S4
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| Molecular Weight |
232.36936
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| Exact Mass |
231.926
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| CAS # |
20362-54-3
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| PubChem CID |
357976
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| Appearance |
White to off-white solid powder
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| LogP |
3.399
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
130
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MZIWZDMEFARRSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H4N2S4/c1-3-9-5(7-1)11-12-6-8-2-4-10-6/h1-4H
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| Chemical Name |
2-(1,3-thiazol-2-yldisulfanyl)-1,3-thiazole
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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 (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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~215.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.76 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 25.0 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: ≥ 2.5 mg/mL (10.76 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 25.0 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: ≥ 2.5 mg/mL (10.76 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 | 4.3035 mL | 21.5174 mL | 43.0348 mL | |
| 5 mM | 0.8607 mL | 4.3035 mL | 8.6070 mL | |
| 10 mM | 0.4303 mL | 2.1517 mL | 4.3035 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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