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Darapladib

Name: Darapladib
Brand: TargetMol
SKU: T6109
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6109Cas No. 356057-34-6

Alias SB-480848

Darapladib (SB-480848) is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 value of 0.25 nM, which can exert cardiovascular protective effects [1,3].

Darapladib

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Purity: 99.88%

Catalog No. T6109Alias SB-480848Cas No. 356057-34-6

Darapladib (SB-480848) is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 value of 0.25 nM, which can exert cardiovascular protective effects [1,3].

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$79	In Stock	In Stock
10 mg	$127	In Stock	In Stock
25 mg	$189	In Stock	In Stock
50 mg	$326	In Stock	In Stock
100 mg	$525	In Stock	In Stock
200 mg	$748	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$118	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.88%

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Darapladib (SB-480848) is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 value of 0.25 nM, which can exert cardiovascular protective effects [1,3].
Targets&IC50	Lp-PLA2:0.25 nM
In vitro	METHODS: Bone marrow-derived macrophages (BMDM) were primed with LPS (100 ng/mL) for 3 h, then treated with 100 nM Darapladib (SB-480848) for 1 h, followed by Ang II (100 nmol/L) treatment for the indicated times. RESULTS Darapladib (SB-480848) attenuated Ang II-induced NLRP3 inflammasome activation and IL-1β production in cardiac macrophages. [3]
In vivo	METHODS: Atherosclerotic Sprague-Dawley rats were fed a high-cholesterol diet for 10 weeks, followed by oral administration of low-dose Darapladib (SB-480848) (25 mg·kg-1·d-1) and high-dose Darapladib ( SB-480848) (50 mg·kg-1·d-1) intervention. RESULTS Serum triglycerides, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), high-sensitivity C-reactive protein (hs-CRP) in the atherosclerosis model group ) and Lp-PLA2 levels were significantly increased, Rho kinase activity and cardiomyocyte apoptosis were also significantly increased (p<0.05 vs. sham operation group), while nitric oxide (NO) production was decreased; Darapladib (SB-480848 ) TC, LDL-C, CRP, Lp-PLA2, and Rho kinase activities were reduced in each group, and NO production was increased; compared with the low-dose Darapladib (SB-480848) group, TC, LDL -C, CRP, and Lp-PLA2 decreased more significantly (p<0.05), and NO production increased more significantly (p<0.05). Compared with the low-dose Darapladib (SB-480848) group, cardiomyocyte apoptosis in the high-dose Darapladib (SB-480848) group was also significantly reduced (p<0.05). However, there was no significant difference in Rho kinase activity between the low-dose Darapladib (SB-480848) group and the high-dose Darapladib (SB-480848) group (p>0.05). [2]
Synonyms	SB-480848

Chemical Properties

Molecular Weight	666.77
Formula	C₃₆H₃₈F₄N₄O₂S
Cas No.	356057-34-6
Smiles	C(C(N(CC1=CC=C(C=C1)C2=CC=C(C(F)(F)F)C=C2)CCN(CC)CC)=O)N3C4=C(C(=O)N=C3SCC5=CC=C(F)C=C5)CCC4
Relative Density.	1.259g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 123.75 mg/mL (185.6 mM), Sonication is recommended.

Ethanol: 93 mg/mL (139.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4998 mL	7.4988 mL	14.9977 mL	74.9884 mL
5 mM	0.3000 mL	1.4998 mL	2.9995 mL	14.9977 mL
10 mM	0.1500 mL	0.7499 mL	1.4998 mL	7.4988 mL
20 mM	0.0750 mL	0.3749 mL	0.7499 mL	3.7494 mL
50 mM	0.0300 mL	0.1500 mL	0.3000 mL	1.4998 mL
100 mM	0.0150 mL	0.0750 mL	0.1500 mL	0.7499 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc