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Elarofiban (Synonyms: RWJ-53308, RWJ53308, RWJ 53308)

Catalog No. T27250 Copy Product Info
Purity: 98.76%
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Elarofiban(RWJ-53308) is a novel and orally active GPIIb/IIIa antagonist.

Elarofiban

Copy Product Info
🥰Excellent
Catalog No. T27250
Synonyms RWJ-53308, RWJ53308, RWJ 53308

Elarofiban(RWJ-53308) is a novel and orally active GPIIb/IIIa antagonist.

Elarofiban
Cas No. 198958-88-2
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$397In StockIn Stock
5 mg$970In StockIn Stock
10 mg$1,290-In Stock
25 mg$1,950-In Stock
50 mg$2,620-In Stock
100 mg$3,530-In Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:98.76%
ee:99.66%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
Elarofiban(RWJ-53308) is a novel and orally active GPIIb/IIIa antagonist.
In vitro
Elarofiban (RWJ-53308) is a novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist that inhibits fibrinogen binding to GPIIb/IIIa with an IC(50) of 0.4+/-0.3 nM. RWJ-53308 inhibits thrombin-induced platelet aggregation in human gel-filtered platelets (IC(50)=60+/-12 nM) and platelet aggregation in human platelet-rich plasma (PRP) in response to collagen, arachidonic acid, ADP, and SFLLRN-NH(2) (IC(50)=60+/-10, 150+/-30, 70+/-4, and 160+/-80 nM, respectively).[4]
In vivo
The potency of Elarofiban (RWJ-53308) in dog and guinea pig PRP is similar to human PRP. RWJ-53308 inhibits ex vivo collagen- and ADP-induced platelet aggregation in conscious dogs for up to 4 h following 0.3 mg/kg iv, and through 4 and 6 h following 1 and 3 mg/kg po. Oral bioavailability is 16+/-7%. RWJ-53308 reduces thrombus weight in a canine arteriovenous (AV) shunt model following intravenous (0.01-0.1 mg/kg) and oral (3 mg/kg) administration. In a guinea pig carotid artery pinch-injury model, RWJ-53308 completely suppresses thrombus-induced cyclic flow reductions (CFR) at 0.7 mg/kg iv. RWJ-53308 also blocks thrombus formation in photoactivation- and ferric chloride-induced models of thrombosis in guinea pigs at 0.3 and 1 mg/kg iv, respectively. In summary, RWJ-53308 is a potent orally active GPIIb/IIIa antagonist that may be useful for both acute and chronic treatment of arterial thrombotic disorders.[4]
SynonymsRWJ-53308, RWJ53308, RWJ 53308
Chemical Properties
Molecular Weight416.51
FormulaC22H32N4O4
Cas No.198958-88-2
Smiles[C@H](NC(=O)[C@H]1CN(C(CCC2CCNCC2)=O)CCC1)(CC(O)=O)C=3C=CC=NC3
Relative Density.1.203 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/mL (144.05 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4009 mL12.0045 mL24.0090 mL120.0451 mL
5 mM0.4802 mL2.4009 mL4.8018 mL24.0090 mL
10 mM0.2401 mL1.2005 mL2.4009 mL12.0045 mL
20 mM0.1200 mL0.6002 mL1.2005 mL6.0023 mL
50 mM0.0480 mL0.2401 mL0.4802 mL2.4009 mL
100 mM0.0240 mL0.1200 mL0.2401 mL1.2005 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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