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Elinogrel

Name: Elinogrel
Brand: TargetMol
SKU: T11177
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11177Cas No. 936500-94-6

Alias PRT060128

Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.

Elinogrel

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Purity: 98.78%

Catalog No. T11177Alias PRT060128Cas No. 936500-94-6

Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$173	In Stock	In Stock
50 mg	$248	In Stock	In Stock
100 mg	$347	In Stock	In Stock
200 mg	$496	-	In Stock
1 mL x 10 mM (in DMSO)	$74	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:98.78%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Elinogrel AI Summary

Elinogrel exhibits a broad spectrum of bioactivities, notably as a P2Y12 receptor antagonist and antiviral agent. It effectively inhibits ADP-stimulated platelet aggregation in human platelet-rich plasma with an IC50 of 2810.0 nM, and displaces [33P]2-MeS-ADP from human recombinant P2Y12 receptors (Ki = 23.0 nM) expressed in CHO cell membranes. Furthermore, it displays high plasma protein binding percentages of 99.31% in dog plasma and 99.58% in human plasma, suggesting a strong binding affinity which may impact its pharmacokinetics. In addition to its antiplatelet activity, Elinogrel shows antiviral activity against SARS-CoV-2 by inhibiting virus-induced cytotoxicity in both Caco-2 and VERO-6 cell lines at a concentration of 10 µM, albeit with variable efficiency. It also demonstrates inhibitory effects on SARS-CoV-2 3CL-Pro protease at 20 µM with an inhibition percentage of 12.48%. The compound's activity extends to enzymatic inhibition, particularly of human HDAC6, where it shows a higher inhibition percentage using commercial peptide substrates (32.69%) compared to custom peptides (1.34%). Additionally, its interaction with various GPCR targets in beta-arrestin recruitment assays reveals inhibitory and activatory actions on multiple receptors such as FFAR4, APLNR, GPR35, and others. Lastly, thermal shift assays and cell viability studies suggest that Elinogrel interacts differently with various protein domains, affecting their stability and function, with mixed bioactivity profiles across different cell types. This highlights its potential versatility and the need for further investigation into its specific mechanisms of action..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.
Targets&IC50	P2Y12:20 nM
Synonyms	PRT060128

Chemical Properties

Molecular Weight	523.95
Formula	C₂₀H₁₅ClFN₅O₅S₂
Cas No.	936500-94-6
Smiles	CNc1cc2[nH]c(=O)n(-c3ccc(NC(=O)NS(=O)(=O)c4ccc(Cl)s4)cc3)c(=O)c2cc1F
Relative Density.	1.31g/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

DMSO: 120 mg/mL (229.03 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.63 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9086 mL	9.5429 mL	19.0858 mL	95.4290 mL
5 mM	0.3817 mL	1.9086 mL	3.8172 mL	19.0858 mL
10 mM	0.1909 mL	0.9543 mL	1.9086 mL	9.5429 mL
20 mM	0.0954 mL	0.4771 mL	0.9543 mL	4.7714 mL
50 mM	0.0382 mL	0.1909 mL	0.3817 mL	1.9086 mL
100 mM	0.0191 mL	0.0954 mL	0.1909 mL	0.9543 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