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| ln Vitro |
The active R-enantiomer of CP-497485 is CP-610431. Rat ACC1 (IC50=35.7 nM) and ACC2 (IC50=55 nM) are more effectively inhibited by CP-610431 than by the racemate CP-497485, but the S-enantiomer CP-610432 does not significantly inhibit either ACC isoform at doses as high as 3 μM. When it comes to preventing HepG2 cell fatty acid and triglyceride (TG) synthesis as well as TG and apoB secretion, CP-610431 is more effective than CP-497485[1]. With EC50s of 1.6, 1.8, 3.0, and 5.7 μM, CP-610431 inhibits the synthesis of fatty acids, triglycerides, TG, and apolipoprotein B in HepG2 cells (ACC1), but not the synthesis of cholesterol or the secretion of apolipoprotein CIII[1]. With nearly comparable potency, CP-610431 suppresses the ACC activity in the liver and skeletal muscle of all three species (rat, 36 versus 55 nM; mouse, 50 against 63 nM; cynomolgus macaque, 70 versus 26 nM) [1]. With IC50 values of 0.11 and 1.2 μM, CP -610431 suppresses the production of fatty acids and TG in mouse primary hepatocytes, whereas its IC50 value for TG secretion is 10 μM[1].
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| ln Vivo |
CP-610431, with ED50s of 22 and 4 mg/kg, respectively, decreases the production of fatty acids in CD1 mice and ob/ob mice within 1 hour after dosing[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HepG2 cells Tested Concentrations: 0.1, 1, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependently inhibited HepG2 cell fatty acid synthesis with an IC50 of 1.6 μM, TG synthesis with an IC50 of 1.8 μM, TG secretion with an IC50 of 3.0 μM, and apoB secretion with an IC50 of 5.7 μM. |
| Animal Protocol |
Animal/Disease Models: CD1 mice[1]
Doses: 30 and 100 mg/ kg for fasting CD1 mice; 10, 30, and 100 mg/kg for non-fasting CD1 mice Route of Administration: intraperitoneal (ip) administration; 1 hour Experimental Results: Inhibited hepatic fatty acid synthesis in fasting CD1 mice by 64±12%, and 77±4% Inhibited hepatic fatty acid synthesis in non-fasting CD1 mice by 18%, 51%, and 75% at doses of 30 and 100 mg/kg, respectively. |
| References |
[1]. H James Harwood Jr, et al. Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in exper
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| Molecular Formula |
C30H37N3O2
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|---|---|
| Molecular Weight |
471.63
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| CAS # |
591778-83-5
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| SMILES |
N1(C2CCN(C(C3=C4C=CC=CC4=CC4=C3C=CC=C4)=O)CC2)CCC[C@@H](C(N(CC)CC)=O)C1
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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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1203 mL | 10.6015 mL | 21.2031 mL | |
| 5 mM | 0.4241 mL | 2.1203 mL | 4.2406 mL | |
| 10 mM | 0.2120 mL | 1.0602 mL | 2.1203 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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