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Vorapaxar

Name: Vorapaxar
Brand: TargetMol
SKU: T7013
Price: 68 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: SCH 530348, MK-5348) Copy Product Info

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Synonyms: SCH 530348, MK-5348

Catalog No. T7013 Copy Product Info

Purity: 99.93%

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Vorapaxar (MK-5348) is a selective, orally active, and competitive antagonist of the plasminogen activator receptor (PAR-1) with a Ki value of 8.1 nM. Vorapaxar primarily acts by targeting PAR-1 on the platelet surface to block thrombin-induced platelet activation. Vorapaxar is suitable for use in cardiovascular disease research.

Cas No. 618385-01-6

Pack Size	Price	USA Stock	Global Stock
1 mg	$68	In Stock	In Stock
5 mg	$148	In Stock	In Stock
10 mg	$213	In Stock	In Stock
25 mg	$363	In Stock	In Stock
50 mg	$497	In Stock	In Stock
100 mg	$713	In Stock	In Stock
200 mg	$986	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$163	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.93%

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Vorapaxar (MK-5348) is a selective, orally active, and competitive antagonist of the plasminogen activator receptor (PAR-1) with a Ki value of 8.1 nM. Vorapaxar primarily acts by targeting PAR-1 on the platelet surface to block thrombin-induced platelet activation. Vorapaxar is suitable for use in cardiovascular disease research.
Targets & IC50	PAR1:8.1 nM (Ki)
In vitro	Methods: Fluorescent calcium indicator Fluo-3/AM was loaded into hPAR1/CHO-K1 cells. After 10-minute preincubation with Vorapaxar, stimuli were added: FXa (0.03 U/mL), thrombin (0.003 U/mL), or PAR1 agonist SFLLRN-NH₂ (3 nM). Fluorescence intensity changes were monitored in real-time using FLIPR. Results: The Ca²⁺ elevation induced by direct PAR1 activation with SFLLRN-NH₂ was inhibited by Vorapaxar, confirming its antagonistic effect on PAR1. [1]
In vivo	Methods: Eight-week-old ApoEko mice (whose platelets do not express PAR1, used to exclude platelet effects) were divided into two groups, both fed a Western diet. The experimental group received feed supplemented with Vorapaxar (10 mg/kg feed), while the control group did not, for a duration of 4 months. Results: The aortic sinus plaque area and overall aortic lipid deposition (Oil Red O staining) were significantly reduced in the Vorapaxar-treated group. [2] Methods: To investigate Vorapaxar's effects on renal function in diabetic nephropathy, male C57BL/6 mice aged 8-12 weeks were intraperitoneally injected with streptozotocin (STZ) (50 mg/kg, for 5 consecutive days) to induce type 1 diabetes. Four weeks after diabetes induction, oral administration of Vorapaxar (1.75 mg/kg) began, twice weekly for 20 weeks. Results: Diabetic mice in the control group exhibited significantly elevated urinary albumin levels. In contrast, diabetic mice treated with Vorapaxar showed no increase in urinary albumin and demonstrated significantly reduced glomerular damage. [3]
Synonyms	SCH 530348, MK-5348

Chemical Properties

Molecular Weight	492.58
Formula	C₂₉H₃₃FN₂O₄
Cas No.	618385-01-6
Smiles	CCOC(=O)N[C@@H]1CC[C@@H]2[C@H](C[C@@H]3[C@@H]([C@@H](C)OC3=O)[C@H]2\C=C\c2ccc(cn2)-c2cccc(F)c2)C1
Relative Density.	1.24 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: 92 mg/mL (186.77 mM), Sonication is recommended.

DMSO: 257.5 mg/mL (522.76 mM), Sonication is recommended.

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.15 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	2.0301 mL	10.1506 mL	20.3013 mL	101.5064 mL
5 mM	0.4060 mL	2.0301 mL	4.0603 mL	20.3013 mL
10 mM	0.2030 mL	1.0151 mL	2.0301 mL	10.1506 mL
20 mM	0.1015 mL	0.5075 mL	1.0151 mL	5.0753 mL
50 mM	0.0406 mL	0.2030 mL	0.4060 mL	2.0301 mL
100 mM	0.0203 mL	0.1015 mL	0.2030 mL	1.0151 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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