Art. -Nr.: HY-102004

Rilapladib

(Synonyms: SB 659032)

3 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.44%
CAS. Nr.: 412950-08-4
Formel: C₄₀H₃₈F₅N₃O₃S
Molecular Weight:735.81

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Rilapladib Chemical Structure

CAS. Nr.: 412950-08-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Rilapladib (SB 659032) is a selective Lp-PLA₂ (lipoprotein-associated phospholipase A₂) inhibitor with an IC₅₀ of 230 pM^[1]. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist^[2].

IC₅₀ & Target

IC50: 230 pM (Lp-PLA₂)^[1].

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 412950-08-4
Appearance Solid
Molecular Weight 735.81
Formel C₄₀H₃₈F₅N₃O₃S
Color Light yellow to yellow
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
Synonyms

SB 659032
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Comput Struct Biotechnol J

HerpDock: A GUI-based gateway to HSV-1 molecular docking insights. [Abstract]

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
Patent

US20220257599A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3590 mL

6.7952 mL

13.5905 mL

5 mM

0.2718 mL

1.3590 mL

2.7181 mL

10 mM

0.1359 mL

0.6795 mL

1.3590 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.25 mg/mL (3.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shaddinger BC, et al. Platelet aggregation unchanged by lipoprotein-associated phospholipase A₂ inhibition: results from an in vitro study and two randomized phase I trials. PLoS One. 2014 Jan 27;9(1):e83094. [Content Brief]

[2]. Athanasios Papakyriakou, et al. Computational Investigation of Darapladib and Rilapladib Binding to Platelet Activating Factor Receptor. A Possible Mechanism of Their Involvement in Atherosclerosis. International Journal of Chemistry; Vol. 6, No. 1; 2014.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Rilapladib

3 Cited Publications

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Rilapladib

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Publications Citing Use of MedChemExpress (MCE) Rilapladib

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rilapladib

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Lipid Metabolism Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Rilapladib

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rilapladib Related Classifications

HY-102004 Related Classifications