| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Rafigrelide's primary target is 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), an enzyme that converts inactive cortisone to active cortisol in tissues such as the liver and adipose tissue. By inhibiting 11β-HSD1, Rafigrelide reduces local cortisol production, which can improve insulin sensitivity and reduce glucose production.
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| ln Vitro |
In vitro, Rafigrelide inhibits 11β-HSD1 activity. Its activity is assessed in cell-free enzyme assays using purified 11β-HSD1 or cell lysates. It has been shown to inhibit the conversion of cortisone to cortisol, with a potent IC50.
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| ln Vivo |
Specific in vivo activity data for Rafigrelide is not detailed in the provided search results. As an 11β-HSD1 inhibitor, it would be expected to improve glucose metabolism and reduce body weight in animal models of diabetes and obesity. It would be administered orally to animals, and its effects on glucose tolerance, insulin sensitivity, and body weight would be assessed.
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| Enzyme Assay |
The in vitro activity of Rafigrelide is assessed using cell-free 11β-HSD1 enzyme assays. In these assays, 11β-HSD1 enzyme is incubated with its substrate (cortisone) and the cofactor NADPH in the presence of varying concentrations of Rafigrelide. The production of cortisol is measured by HPLC or by using a radioactive assay (e.g., [3H]cortisone). The IC50 is determined as the concentration of Rafigrelide required to inhibit 50% of the enzyme activity.
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| Cell Assay |
For cellular assays, cells expressing 11β-HSD1 (e.g., primary hepatocytes or adipocytes) are used. Cells are treated with various concentrations of Rafigrelide (typically ranging from 1 nM to 10 µM) for different time periods. The conversion of cortisone to cortisol is measured in the culture medium by ELISA or by HPLC. The effect on glucose production can be assessed in hepatocytes by measuring glucose release.
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| Animal Protocol |
In vivo, Rafigrelide is typically administered orally to animal models of metabolic disease, such as diet-induced obese (DIO) mice or db/db mice. The compound is formulated in a suitable vehicle and administered at various doses (e.g., 1-100 mg/kg) once or twice daily. Glucose tolerance tests (GTT) and insulin tolerance tests (ITT) are performed to assess metabolic effects. Body weight, food intake, and adipose tissue mass are measured.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Rafigrelide is not available in the provided search results. As a small molecule with a molecular weight of 420.38 g/mol, it is expected to have reasonable oral bioavailability. Its half-life and metabolism would require further investigation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Rafigrelide is not available in the provided search results. As a research compound, its safety profile has not been fully established. Comprehensive toxicological studies are required to assess its safety.
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| Additional Infomation |
Rafigrelide is a research compound used to study the role of 11β-HSD1 in metabolic disorders. It is a tool for investigating the therapeutic potential of 11β-HSD1 inhibitors for the treatment of type 2 diabetes and obesity. It is not approved for clinical use.
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| Molecular Formula |
C12H11CL2N3O
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|---|---|
| Molecular Weight |
284.1412
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| Exact Mass |
283.028
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| CAS # |
1029711-88-3
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| PubChem CID |
135564921
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.354
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
424
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C([H])=C([H])C2=C1C([H])([H])N1C(=N2)N([H])C(C1(C([H])([H])[H])C([H])([H])[H])=O)Cl
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| InChi Key |
IGMDPBNGNRHCRW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H11Cl2N3O/c1-12(2)10(18)16-11-15-8-4-3-7(13)9(14)6(8)5-17(11)12/h3-4H,5H2,1-2H3,(H,15,16,18)
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| Chemical Name |
6,7-dichloro-3,3-dimethyl-1,5-dihydroimidazo[2,1-b]quinazolin-2-one
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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 |
| 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 : ~1.11 mg/mL (~3.91 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 | 3.5194 mL | 17.5970 mL | 35.1939 mL | |
| 5 mM | 0.7039 mL | 3.5194 mL | 7.0388 mL | |
| 10 mM | 0.3519 mL | 1.7597 mL | 3.5194 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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