P053 |
| カタログ番号GC44529 |
P053 は、0.5 μM の IC50 を持つ、強力で非競合的かつ選択的なセラミド合成酵素 1 (CerS1) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2748196-63-4
Sample solution is provided at 25 µL, 10mM.
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P053 is an inhibitor of ceramide synthase 1 (CerS1; IC50s = 0.54 and 0.46 µM for human and mouse CerS1, respectively). It is selective for CerS1 over CerS2, CerS4, CerS5, and CerS6 (IC50s = 28.6, 17.2, 7.2, and 11.4 µM, respectively). P053 decreases the production of C18 ceramide from dihydrosphingosine in cortical neuron cultures in a concentration-dependent manner. It also lowers levels of C18 ceramide, C18 galactosylceramide, and C18:0 and 18:1 sphingomyelin species in HEK293 cells, when used at concentrations ranging from 30 to 300 nM, without inducing cell death. P053 (5 mg/kg) decreases endogenous C18 and C18:2/18:0 ceramide levels and increases C22:0 , C24:0 , and C24:1 ceramide levels in mouse skeletal muscle. It increases fatty acid oxidation in mouse skeletal muscle and inhibits triglyceride synthesis and increases in white adipose mass in a model of high-fat diet-induced obesity but does not affect insulin resistance.
| Cas No. | 2748196-63-4 | SDF | |
| Canonical SMILES | ClC1=C(Cl)C=C(COC2=CC=C(CC[C@@](N)(C)CO)C=C2)C=C1 | ||
| Formula | C18H21Cl2NO2 | M.Wt | 354.3 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8225 mL | 14.1123 mL | 28.2247 mL |
| 5 mM | 0.5645 mL | 2.8225 mL | 5.6449 mL |
| 10 mM | 0.2822 mL | 1.4112 mL | 2.8225 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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