Rilapladib (Synonyms: SB 659032)

Name: Rilapladib
Brand: MedChemExpress
SKU: HY-102004
Rating: 5.0 (2 reviews)

Cat. No.: HY-102004 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Rilapladib Chemical Structure

CAS No. : 412950-08-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 469	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 469	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 470	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 940	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Rilapladib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phospholipase Isoform Specific Products:

View All Isoforms

Phospholipase A PLD Phospholipase C

Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

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

Molecular Weight

735.81

Formula

C₄₀H₃₈F₅N₃O₃S

CAS No.

412950-08-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (283 KB) SDS (251 KB)

COA (251 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

Neurological Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rilapladib412950-08-4SB 659032SB659032SB-659032PhospholipaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Rilapladib (Synonyms: SB 659032)

Customer Review

Rilapladib Related Antibodies

2 Publications Citing Use of MCE Rilapladib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phospholipase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Rilapladib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rilapladib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report