Rilapladib
Based on 3 publication(s) in Google Scholar
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.44%
- No. CAS: 412950-08-4
- Fòrmula: C40H38F5N3O3S
- Peso molecular:735.81
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Rilapladib
MoreVer todos los productos específicos de isoformas Phospholipase
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Actividad biológica
IC50: 230 pM (Lp-PLA2)[1].
Rilapladib through reduction of the PAF biological activity (as PAF inhibitors) and PAF levels could reduce Lp-PLA2 biosynthesis and prevent the possible adverse effects of Lp-PLA2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 412950-08-4
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Appearance Solid
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Peso molecular 735.81
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Fòrmula C40H38F5N3O3S
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Color Light yellow to yellow
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SMILES
O=C(N(C1CCN(CCOC)CC1)CC2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)CN4C(SCC5=CC=CC(F)=C5F)=CC(C6=C4C=CC=C6)=O
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Synonyms
SB 659032
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Comput Struct Biotechnol J
2024 Oct 13:23:3692-3701. PMID: 39507821 -
ACS Chem Biol
Phospholipase PAFAH2 Mediates Ferroptosis Surveillance and Lipid Remodeling to Promote Resistance in KEAP1 Mutant Cancers. [Abstract]2025 Jul 18;20(7):1739-1755. PMID: 40600963 -
Solvente y solubilidad
DMSO : 86.67 mg/mL (117.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.25 mg/mL (3.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.25 mg/mL (3.06 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.3590 mL | 6.7952 mL | 13.5905 mL | 33.9762 mL |
| 5 mM | 0.2718 mL | 1.3590 mL | 2.7181 mL | 6.7952 mL | |
| 10 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | 3.3976 mL | |
| 15 mM | 0.0906 mL | 0.4530 mL | 0.9060 mL | 2.2651 mL | |
| 20 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 25 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3590 mL | |
| 30 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1325 mL | |
| 40 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL | |
| 50 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 60 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL | |
| 80 mM | 0.0170 mL | 0.0849 mL | 0.1699 mL | 0.4247 mL | |
| 100 mM | 0.0136 mL | 0.0680 mL | 0.1359 mL | 0.3398 mL |
Rilapladib Related Classifications
HY-102004 Related Classifications
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