| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
BE1218 targets liver X receptors (LXRs), specifically LXRα and LXRβ, which are nuclear receptors that regulate cholesterol, lipid, and glucose metabolism as well as inflammatory responses. BE1218 is an LXR inverse agonist with IC50 values of 9 nM against LXRα and 7 nM against LXRβ. As an inverse agonist, it stabilizes the receptor in an inactive conformation, reducing basal transcriptional activity.
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| ln Vitro |
In vitro, BE1218 is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM against LXRα and 7 nM against LXRβ. It is active on both LXR isoforms. These in vitro properties make BE1218 a valuable tool for studying LXR function, including its roles in lipid metabolism, cholesterol homeostasis, inflammation, and cancer.
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| ln Vivo |
In vivo activity of BE1218 has not been extensively reported. As an LXR inverse agonist, it may have potential for treating metabolic diseases, inflammatory conditions, or cancer. However, detailed in vivo efficacy data are limited in publicly available sources. The compound is primarily used as a research tool for studying LXR biology.
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| Enzyme Assay |
The in vitro receptor binding assay for BE1218 involves measuring its binding affinity to LXRα and LXRβ. The compound is incubated with recombinant LXR proteins in the presence of a labeled LXR ligand. Binding affinity is determined using fluorescence polarization, surface plasmon resonance, or radioligand binding assays. Functional activity as an inverse agonist is assessed by measuring LXR-mediated transcriptional activity in reporter gene assays.
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| Cell Assay |
The in vitro cell-based assay for BE1218 involves culturing cells expressing LXRα or LXRβ and treating them with the compound to assess effects on LXR transcriptional activity. Cells are transfected with an LXR-responsive reporter plasmid and treated with BE1218 at various concentrations. Reporter gene activity (e.g., luciferase) is measured to determine the IC50 for LXR inhibition. Target gene expression (e.g., ABCA1, SREBP-1c) can be assessed by qPCR. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for BE1218 have not been extensively reported. If conducted, such studies might involve mouse models of metabolic diseases, inflammation, or cancer. BE1218 would be administered orally or intraperitoneally, and metabolic parameters, inflammatory markers, or tumor growth would be assessed. Standard protocols for these models would be employed. No specific data are available.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of BE1218 have not been extensively characterized. As a small molecule with a molecular weight of 551.69 and a molecular formula of C30H30FNO4S2, it is expected to have moderate oral bioavailability. The compound is soluble in DMSO and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of BE1218 has not been systematically evaluated. As an LXR inverse agonist, its primary safety concerns would relate to effects on lipid metabolism and cholesterol homeostasis. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
BE1218 is a research compound and has not been approved for clinical use. It is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM against LXRα and 7 nM against LXRβ. BE1218 is a valuable tool for studying LXR function, including its roles in lipid metabolism, cholesterol homeostasis, inflammation, and cancer.
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| Molecular Formula |
C30H30FNO4S2
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|---|---|
| Molecular Weight |
551.691909313202
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| Exact Mass |
551.16
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| Elemental Analysis |
C, 65.31; H, 5.48; F, 3.44; N, 2.54; O, 11.60; S, 11.62
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| CAS # |
2893967-40-1
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| PubChem CID |
164887446
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| Appearance |
White to off-white solid powder
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| LogP |
6.1
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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 |
8
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| Heavy Atom Count |
38
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| Complexity |
955
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C(C)=CC(C)=CC=1C)(N(CC1C=CC=CC=1F)CC1C=CC(C2C=CC=C(C=2)S(C)(=O)=O)=CC=1)(=O)=O
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| InChi Key |
YZKNHPOMZOAMSW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H30FNO4S2/c1-21-16-22(2)30(23(3)17-21)38(35,36)32(20-27-8-5-6-11-29(27)31)19-24-12-14-25(15-13-24)26-9-7-10-28(18-26)37(4,33)34/h5-18H,19-20H2,1-4H3
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| Chemical Name |
N-(2-fluorobenzyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)benzenesulfonamide
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| Synonyms |
BE1218; BE-1218; BE 1218;
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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 : ~33.33 mg/mL (~60.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8126 mL | 9.0631 mL | 18.1261 mL | |
| 5 mM | 0.3625 mL | 1.8126 mL | 3.6252 mL | |
| 10 mM | 0.1813 mL | 0.9063 mL | 1.8126 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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