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| Targets |
IMB-808 targets liver X receptor α (LXRα) and LXRβ (LXRα/β), nuclear receptors that play a key role in cholesterol metabolism and inflammation. By acting as a partial dual agonist, it modulates the expression of genes involved in reverse cholesterol transport, such as ABCA1 and ABCG1.
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| ln Vitro |
In the concentration range of 0.001 μM to 30 μM, IMB-808 (0.001 μM-30 μM) substantially and dose-dependently stimulates LXRβ activation, with an EC50 of 0.53 μM. Moreover, IMB-808 replicated the activation of LXRα in a luciferase reporter assay with an EC50 of 0.15 μM utilizing the GAL4-pGL4-luc reporter [1]. In RAW264.7 macrophages, IMB-808 (0 μM–10 μM; 18 hours) dramatically raises the protein and mRNA levels of ABCG1 and ABCA1 [1]. In lineage cells, IMB-808 (0.1 μM, 0.3 μM, 1 μM, 3 μM, or 10 μM; 24 hours) depletes cholesterol and decreases the amount of cholesterol in the cells.
In vitro, IMB-808 induces transactivation of LXRα and LXRβ in reporter assays using HEK293T cells, with EC50 values of 0.15 and 0.53 µM, respectively. It promotes ABCA1 expression and cholesterol efflux without inducing lipidogenesis in HepG2 cells, making it a promising candidate for atherosclerosis research. |
| ln Vivo |
In vivo, IMB-808 is being studied for its potential in treating atherosclerosis. By promoting reverse cholesterol transport and reducing inflammation, it may help reduce atherosclerotic plaque formation and progression.
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| Enzyme Assay |
LXR binding affinity is determined using radioligand binding assays. Recombinant LXR proteins are incubated with a radiolabeled ligand and varying concentrations of IMB-808. The Ki values are calculated from competitive binding curves.
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| Cell Assay |
The functional activity of IMB-808 is assessed in cells expressing LXR, such as HEK293T cells transfected with a GAL4-pGL4-luc reporter plasmid. Cells are treated with the compound, and luciferase activity is measured to determine the EC50 for transactivation.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of atherosclerosis, such as ApoE-deficient mice. IMB-808 is administered orally, and atherosclerotic lesion area, plasma lipid profiles, and expression of LXR target genes (e.g., ABCA1, ABCG1) are measured.
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| ADME/Pharmacokinetics |
As a small molecule with a molecular weight of 380.31 g/mol, IMB-808 is expected to have favorable drug-like properties, including good oral bioavailability. Its pharmacokinetic properties are consistent with a small molecule nuclear receptor modulator.
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| Toxicity/Toxicokinetics |
LXR agonists can cause hypertriglyceridemia and hepatic steatosis, which are common side effects of this class. However, IMB-808's partial agonist activity and its ability to promote cholesterol efflux without inducing lipidogenesis in HepG2 cells suggest a potentially improved safety profile.
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| References | |
| Additional Infomation |
IMB-808 is a research compound being developed for the treatment of atherosclerosis. It is a potent LXRα/β partial dual agonist that promotes reverse cholesterol transport without inducing lipidogenesis. It is not approved for clinical use.
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| Molecular Formula |
C18H15F3N2O4
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|---|---|
| Molecular Weight |
380.32
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| Exact Mass |
380.098
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| CAS # |
870768-70-0
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| PubChem CID |
8001903
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
572.8±50.0 °C at 760 mmHg
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| Flash Point |
300.2±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.592
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| LogP |
2.96
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
553
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(CC(=O)NC1=C(C(=C(C=C1)F)F)F)C(=O)C2=CC3=C(C=C2)OCCO3
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| InChi Key |
XITZPIXICJOKTF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15F3N2O4/c1-23(9-15(24)22-12-4-3-11(19)16(20)17(12)21)18(25)10-2-5-13-14(8-10)27-7-6-26-13/h2-5,8H,6-7,9H2,1H3,(H,22,24)
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| Chemical Name |
N-methyl-N-[2-oxo-2-(2,3,4-trifluoroanilino)ethyl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide
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| Synonyms |
IMB808; IMB 808; IMB-808
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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 : ~250 mg/mL (~657.34 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 | 2.6294 mL | 13.1468 mL | 26.2936 mL | |
| 5 mM | 0.5259 mL | 2.6294 mL | 5.2587 mL | |
| 10 mM | 0.2629 mL | 1.3147 mL | 2.6294 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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