| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CKD-519 targets cholesteryl ester transfer protein (CETP), a plasma protein that facilitates the transfer of cholesteryl esters from HDL to LDL and VLDL. By inhibiting CETP, CKD-519 blocks this transfer, leading to increased HDL-C levels and decreased LDL-C levels. CETP inhibition is a therapeutic strategy for the treatment of dyslipidemia and prevention of cardiovascular disease.
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| ln Vitro |
In vitro, CKD-519 potently inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM. It demonstrates high selectivity for CETP over other lipid-modifying enzymes. The compound shows concentration-dependent inhibition of CETP activity in human plasma-based assays. Detailed in vitro characterization including IC50 values, selectivity profile, and mechanism of inhibition are available from published studies.
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| ln Vivo |
In vivo, CKD-519 has been shown to effectively elevate HDL-C levels and reduce LDL-C levels in animal models of dyslipidemia. By inhibiting CETP activity, the compound improves the lipid profile, potentially reducing the risk of cardiovascular disease. CKD-519 has been studied in preclinical models for its efficacy in modulating lipid metabolism. Detailed in vivo data including dose-response relationships and duration of action are available from published studies.
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| Enzyme Assay |
In vitro enzyme assays for CETP inhibition typically use human plasma or recombinant CETP as the enzyme source and a fluorescent or radiolabeled cholesteryl ester donor (e.g., [³H]cholesteryl ester-labeled HDL) and acceptor (LDL or VLDL). The enzyme is incubated with the donor and acceptor in the presence of varying concentrations of CKD-519. The transfer of cholesteryl ester from donor to acceptor is measured by scintillation counting or fluorescence. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for CETP inhibitors are not typically performed as CETP is a plasma protein rather than a cellular target. However, assays using CETP-expressing cell lines or primary hepatocytes may be used to assess the compound's effects on cholesterol efflux and lipid metabolism. Cells are treated with CKD-519, and HDL-mediated cholesterol efflux is measured using radioactive cholesterol labeling. Cellular cholesterol content and lipid profile are also assessed.
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| Animal Protocol |
In vivo animal studies for CETP inhibitors typically use transgenic mouse models expressing human CETP (since mice naturally lack CETP) or hamster models (which have CETP). Animals are administered CKD-519 orally at various doses for a defined treatment period (e.g., 2-4 weeks). Blood samples are collected at baseline and at various time points during treatment. Lipid parameters including total cholesterol, HDL-C, LDL-C, and triglycerides are measured. The percentage change in HDL-C and LDL-C is calculated.
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| ADME/Pharmacokinetics |
CKD-519 is orally bioavailable with good absorption following oral administration. As a small-molecule CETP inhibitor, it distributes to the plasma where it binds to CETP and inhibits its activity. The compound is metabolized in the liver, and its metabolites are excreted primarily via the kidneys and bile. Detailed PK parameters such as half-life, Cmax, Tmax, and AUC are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CKD-519 would typically include acute and repeated-dose toxicity in rodents and dogs, as well as genotoxicity and safety pharmacology assessments. CETP inhibitors as a class have been associated with potential off-target effects, and careful safety evaluation is required. The compound is generally well-tolerated at therapeutic doses. Common side effects may include gastrointestinal disturbances, headache, and flushing. Serious adverse effects are rare.
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| References | |
| Additional Infomation |
Rocacetrapib is being investigated in the clinical trial NCT02156544 (investigating the safety/tolerability and pharmacokinetics/pharmacodynamics of CKD-519).
CKD-519 is a potent and selective CETP inhibitor with an IC50 of 2.3 nM. By inhibiting CETP-mediated cholesteryl ester transfer, it elevates HDL-C and reduces LDL-C levels. CETP inhibition represents a therapeutic strategy for dyslipidemia and cardiovascular disease prevention. CKD-519 has been studied in preclinical models for its lipid-modulating effects. The compound is available for research use only and is not approved for clinical use. |
| Molecular Formula |
C31H34F7NO3
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|---|---|
| Molecular Weight |
601.595393657684
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| Exact Mass |
601.242
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| CAS # |
1402796-27-3
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| PubChem CID |
70674853
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| Appearance |
White to off-white solid powder
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| LogP |
8.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
42
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| Complexity |
986
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| Defined Atom Stereocenter Count |
2
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| SMILES |
FC1C=C(C(=CC=1C(C)C)C1CCC(C)(C)CC=1CN1C(=O)O[C@H](C2C=C(C(F)(F)F)C=C(C(F)(F)F)C=2)[C@@H]1C)OC
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| InChi Key |
GBHPDJQHZADVAA-SOKVYYICSA-N
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| InChi Code |
InChI=1S/C31H34F7NO3/c1-16(2)23-12-24(26(41-6)13-25(23)32)22-7-8-29(4,5)14-19(22)15-39-17(3)27(42-28(39)40)18-9-20(30(33,34)35)11-21(10-18)31(36,37)38/h9-13,16-17,27H,7-8,14-15H2,1-6H3/t17-,27-/m0/s1
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| Chemical Name |
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5,5-dimethylcyclohexen-1-yl]methyl]-4-methyl-1,3-oxazolidin-2-one
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| Synonyms |
CKD519; CKD 519; CKD-519
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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 : ~66.67 mg/mL (~110.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.16 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 | 1.6622 mL | 8.3112 mL | 16.6223 mL | |
| 5 mM | 0.3324 mL | 1.6622 mL | 3.3245 mL | |
| 10 mM | 0.1662 mL | 0.8311 mL | 1.6622 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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