Lp-PLA2-IN-3
Based on 1 Customer Validation
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
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- Pureté: 99.94%
- CAS No.: 2196245-16-4
- Formule: C20H13ClF3N3O3S
- Masse moléculaire:467.85
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Lp-PLA2-IN-3 (1 mg/kg; i.v.) treatment shows the CL, Vss, and t1/2 were 3.1mL/min/kg, 0.3 L/kg, 4 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague−Dawley (SD) rats (180-220 g)[1]
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Dosage:3 mg/kg
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Administration:p.o. (Pharmacokinetic Analysis)
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Result:The Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 6.2 μg h/mL, 7.7 hours and 35.5%, respectively.
Chemical Information
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CAS No. 2196245-16-4
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Appearance Solid
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Masse moléculaire 467.85
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Formule C20H13ClF3N3O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(N)C=C1)(NC2=CC=C(OC3=CC=C(Cl)C(C(F)(F)F)=C3)C(C#N)=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : ≥ 250 mg/mL (534.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1374 mL | 10.6872 mL | 21.3744 mL | 53.4359 mL |
| 5 mM | 0.4275 mL | 2.1374 mL | 4.2749 mL | 10.6872 mL | |
| 10 mM | 0.2137 mL | 1.0687 mL | 2.1374 mL | 5.3436 mL | |
| 15 mM | 0.1425 mL | 0.7125 mL | 1.4250 mL | 3.5624 mL | |
| 20 mM | 0.1069 mL | 0.5344 mL | 1.0687 mL | 2.6718 mL | |
| 25 mM | 0.0855 mL | 0.4275 mL | 0.8550 mL | 2.1374 mL | |
| 30 mM | 0.0712 mL | 0.3562 mL | 0.7125 mL | 1.7812 mL | |
| 40 mM | 0.0534 mL | 0.2672 mL | 0.5344 mL | 1.3359 mL | |
| 50 mM | 0.0427 mL | 0.2137 mL | 0.4275 mL | 1.0687 mL | |
| 60 mM | 0.0356 mL | 0.1781 mL | 0.3562 mL | 0.8906 mL | |
| 80 mM | 0.0267 mL | 0.1336 mL | 0.2672 mL | 0.6679 mL | |
| 100 mM | 0.0214 mL | 0.1069 mL | 0.2137 mL | 0.5344 mL |