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| Targets |
Managlinat dialanetil acts as an inhibitor of fructose-1,6-bisphosphatase (FBPase). FBPase is a key enzyme in the gluconeogenesis pathway, catalyzing the hydrolysis of fructose-1,6-bisphosphate to fructose-6-phosphate. By inhibiting FBPase, managlinat dialanetil reduces the rate of gluconeogenesis in the liver. This leads to a decrease in hepatic glucose output and subsequently lowers blood glucose levels. The compound's mechanism of action is independent of insulin secretion, making it a potential therapeutic option for patients with type 2 diabetes who have impaired insulin secretion or insulin resistance.
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| ln Vitro |
Managlinat dialanetil's in vitro activity is characterized by its potent inhibition of FBPase. As a FBPase inhibitor, it directly targets the enzyme's activity in cell-free systems. The compound's inhibitory potency is reflected in its IC50 value against FBPase. In vitro studies have demonstrated its ability to effectively inhibit the enzyme's catalytic function, which is the basis for its hypoglycemic effects in vivo.
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| ln Vivo |
In Zucker diabetic fat (ZDF) rats, managlinat dialanetil dose-dependently suppresses GNG and lowers baseline and postprandial blood glucose levels [1].
Managlinat dialanetil demonstrates significant in vivo activity by lowering blood glucose levels. In Zucker diabetic fatty (ZDF) rats, a model of type 2 diabetes, managlinat dialanetil dose-dependently suppresses gluconeogenesis (GNG). Oral administration of the compound lowers both baseline and postprandial blood glucose levels in these animals. These findings support its potential as a therapeutic agent for managing hyperglycemia in type 2 diabetes. The compound has also been evaluated in Phase II clinical trials for its glucose-lowering effect, safety, and tolerability in humans. |
| Enzyme Assay |
In vitro enzyme assays for managlinat dialanetil typically measure its ability to inhibit FBPase activity. The enzyme is incubated with its substrate, fructose-1,6-bisphosphate, in the presence of increasing concentrations of the compound. The production of fructose-6-phosphate is then measured using spectrophotometric or coupled enzyme assays. IC50 values are calculated from dose-response curves to quantify the compound's potency as an FBPase inhibitor.
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| Cell Assay |
Cell-based assays for managlinat dialanetil are not commonly used, as its primary mechanism of action is through enzyme inhibition in the liver. However, its effects on gluconeogenesis can be studied in hepatocyte cultures. Primary hepatocytes or liver cell lines are treated with the compound, and glucose production is measured. The compound's ability to inhibit gluconeogenesis in these cellular models is assessed, providing further evidence of its mechanism of action.
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| Animal Protocol |
In vivo animal studies for managlinat dialanetil are conducted in models of type 2 diabetes, such as the ZDF rat model. The compound is administered orally, and its effects on blood glucose levels, both baseline and postprandial, are measured. Pharmacokinetic studies are also performed to evaluate its absorption, distribution, metabolism, and excretion. These studies are essential for determining the compound's efficacy, safety, and dosing regimen.
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| ADME/Pharmacokinetics |
Managlinat dialanetil (CAS 280782-97-0) has a molecular formula of C21H33N4O5PS and a molecular weight of 484.55 g/mol. It is a white to yellow solid powder. The compound is soluble in DMSO at approximately 25 mg/mL. For storage, the powder should be kept at -20°C, where it is stable for up to 3 years. In solution, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound has a LogP of 2.57. It should be stored in a sealed and protected environment, such as under nitrogen, to avoid exposure to moisture.
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| Toxicity/Toxicokinetics |
The toxicological profile of managlinat dialanetil has been evaluated in preclinical and clinical studies. In Phase II clinical trials, its safety and tolerability were assessed. As an investigational drug, its full safety profile is not yet fully established. It is intended for research use only and is not for human or veterinary use.
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| References | |
| Additional Infomation |
CS-917 is a novel fructose-1,6-bisphosphatase (FBPase) inhibitor, one of the rate-limiting enzymes in the gluconeogenesis pathway.
Drug Indications It has been investigated for the treatment of type 2 diabetes.Mechanism of Action In type 2 diabetes, the liver produces excess glucose through the gluconeogenesis (GNG) pathway, leading to the characteristic hyperglycemia of the disease. CS-917 targets the AMP binding site of fructose-1,6-bisphosphatase (FBPase), thereby inhibiting the gluconeogenesis pathway. Managlinat dialanetil (MB06322, CS-917) is an orally bioavailable inhibitor of fructose-1,6-bisphosphatase (FBPase). It was developed for the treatment of type 2 diabetes mellitus. The compound has been investigated in Phase II clinical trials for its glucose-lowering effects. It is also known by the synonyms CS-917, GP-3034, MB-05032, MB-06322, MB-06633, and MB-6322. Managlinat dialanetil is a valuable research tool for studying the role of gluconeogenesis in glucose homeostasis and for developing new therapeutic strategies for type 2 diabetes. It is not approved for clinical use. |
| Molecular Formula |
C21H33N4O5PS
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|---|---|
| Molecular Weight |
484.55
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| Exact Mass |
500.185
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| CAS # |
280782-97-0
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| PubChem CID |
9811837
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
634.8±65.0 °C at 760 mmHg
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| Flash Point |
337.7±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.552
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| LogP |
2.57
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
33
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| Complexity |
684
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| Defined Atom Stereocenter Count |
2
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| Synonyms |
Managlinat dialanetil; MB-06322, MB 06322, MB06322, CS-917, CS 917, CS917
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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 : ~25 mg/mL (~49.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0638 mL | 10.3189 mL | 20.6377 mL | |
| 5 mM | 0.4128 mL | 2.0638 mL | 4.1275 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0638 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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