| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
CP-868388 targets the peroxisome proliferator-activated receptor alpha (PPARα), a nuclear receptor that regulates lipid metabolism and inflammation. It acts as a selective PPARα agonist. The compound exhibits sub-nanomolar binding affinity for human PPARα (Ki = 10.8 nM) and is highly selective over other PPAR isoforms, showing little or no affinity for PPARβ (Ki = 3.47 μM) and PPARγ.
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| ln Vitro |
CP-868388 (0-1 mM) demonstrates strong and dose-dependent recruitment of SRC-1 (EC50 of 4.7 nM) and PGC-1α peptide [1]. CP-868388 displays strong and selective stimulation of PPARα transcription in HepG2 cells with an EC50 of 18 nM [1].
In vitro, CP-868388 demonstrates potent and selective transcriptional activation of PPARα. In cell-based assays using HepG2 cells, it shows an EC50 of 18 nM for PPARα transcriptional activation. The compound also exhibits strong and dose-dependent recruitment of the coactivator peptides SRC-1 and PGC-1α, with EC50 values of 4.7 nM. This activity is consistent with its role as a potent PPARα agonist. |
| ln Vivo |
Treatment with CP-868388 (0-3 mg/kg; oral gavage; once daily; for 2 days; male B6/CBF1J mice) demonstrated a significant reduction in circulating plasma triglycerides. The lowering of triglycerides is dose-dependent, with the highest impact at a dose of 3.0 mg/kg, with triglycerides lowered by nearly 50% [1].
In vivo, oral administration of CP-868388 in male B6/CBF1J mice results in a robust and dose-dependent decrease in circulating plasma triglycerides. Doses ranging from 0 to 3 mg/kg, administered once daily for two days, achieved the greatest efficacy at 3.0 mg/kg, leading to a reduction of approximately 50% in triglyceride levels. This demonstrates its potent lipid-modifying effects in preclinical models. |
| Enzyme Assay |
In cell-free biochemical assays, CP-868388's activity is typically evaluated by measuring its binding affinity for PPARα. The assay involves incubating the purified human PPARα ligand-binding domain (LBD) with a fluorescently labeled tracer and varying concentrations of the test compound. The displacement of the tracer is measured, and the Ki value (10.8 nM) is calculated from the competition curve.
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| Cell Assay |
In vitro cell-based experiments with CP-868388 typically use HepG2 cells, a human liver cancer cell line. Cells are transfected with a PPARα-responsive luciferase reporter construct and treated with various concentrations of the compound. After incubation, the luciferase activity is measured, and the EC50 for transcriptional activation (18 nM) is determined from the concentration-response curve.
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| Animal Protocol |
Animal/Disease Models: Male B6/CBF1J mice[1]
Doses: 0 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg Route of Administration: po (oral gavage); one time/day; for 2 days Experimental Results: Circulation Plasma triglycerides were Dramatically diminished. In vivo animal experiments are conducted in male B6/CBF1J mice. Mice are administered CP-868388 via oral gavage at doses ranging from 0 to 3 mg/kg, once daily for two days. Blood samples are collected, and plasma triglyceride levels are measured to assess the compound's lipid-lowering efficacy. |
| ADME/Pharmacokinetics |
CP-868388 is an orally active compound with robust oral bioavailability. In pharmacokinetic studies, it has demonstrated favorable properties, including a Cmax of 3.0 and an AUC of 8, with an oral bioavailability (F) of 53%. Its molecular weight is 439.54 g/mol.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CP-868388 beyond standard safety precautions for research chemicals. Material Safety Data Sheets indicate that under fire conditions, it may decompose and emit toxic fumes. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
CP-868388 has a molecular formula of C26H33NO5 and a molecular weight of 439.54 g/mol. It is also known by the synonyms UNII-999KY5ZIGB, CP868388, and (-)-CP-868388. The compound is a potent and selective PPARα agonist, providing over 320-fold selectivity over PPARβ/γ. It is a valuable research tool for studying PPARα-mediated lipid metabolism, inflammation, and dyslipidemia. It is not approved for clinical use.
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| Molecular Formula |
C26H33NO5
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| Molecular Weight |
439.54
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| Exact Mass |
439.236
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| CAS # |
702681-67-2
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| PubChem CID |
10433320
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| Appearance |
White to off-white solid powder
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| LogP |
5.506
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
626
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)C1=CC=C(C=C1)COC(=O)N2CCC[C@H](C2)C3=CC(=CC=C3)OC(C)(C)C(=O)O
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| InChi Key |
CSLFIHDRJSTULR-JOCHJYFZSA-N
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| InChi Code |
InChI=1S/C26H33NO5/c1-18(2)20-12-10-19(11-13-20)17-31-25(30)27-14-6-8-22(16-27)21-7-5-9-23(15-21)32-26(3,4)24(28)29/h5,7,9-13,15,18,22H,6,8,14,16-17H2,1-4H3,(H,28,29)/t22-/m1/s1
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| Chemical Name |
2-methyl-2-[3-[(3S)-1-[(4-propan-2-ylphenyl)methoxycarbonyl]piperidin-3-yl]phenoxy]propanoic acid
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| Synonyms |
CP 868388 CP868388 CP-868388
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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 : ~125 mg/mL (~284.39 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 | 2.2751 mL | 11.3755 mL | 22.7511 mL | |
| 5 mM | 0.4550 mL | 2.2751 mL | 4.5502 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2751 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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