| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Elinogrel targets the P2Y12 receptor on platelets. As a competitive and reversible antagonist, it binds to the P2Y12 receptor and prevents adenosine diphosphate (ADP) from binding to its platelet receptor. This inhibits ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby preventing platelet aggregation. The compound is selective for P2Y12 and directly inhibits platelet function without requiring metabolic activation.
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| ln Vitro |
In vitro, Elinogrel is a potent P2Y12 antagonist with an IC50 of 20 nM. It directly inhibits ADP-induced platelet aggregation in a concentration-dependent manner. As a reversible inhibitor, its effects are dependent on the presence of the compound and can be overcome by high concentrations of ADP. The compound shows potent antiplatelet activity comparable to or greater than other P2Y12 inhibitors.
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| ln Vivo |
In vivo, Elinogrel has been investigated for the prevention of thrombotic events in patients with acute coronary syndrome (ACS) and those undergoing percutaneous coronary intervention (PCI). It is effective in reducing the risk of cardiovascular events such as myocardial infarction, stroke, and death in these patient populations. Both oral and intravenous formulations have been studied. The compound's reversible binding may offer advantages over irreversible P2Y12 inhibitors in terms of bleeding risk management.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Elinogrel measure binding to the P2Y12 receptor using radioligand binding (e.g., [³H]2-MeS-ADP) in platelet membrane preparations. Competition binding experiments are performed with various concentrations of Elinogrel to calculate IC50 or Ki values. Functional assays measure inhibition of ADP-induced platelet aggregation in platelet-rich plasma using a platelet aggregometer. The IC50 for inhibition of aggregation is determined from dose-response curves.
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| Cell Assay |
Cellular assays for Elinogrel use human or rodent platelets isolated from whole blood. Platelet-rich plasma (PRP) is prepared and treated with various concentrations of Elinogrel. Platelet aggregation is induced by ADP, and aggregation is measured using light transmission aggregometry or impedance aggregometry. P2Y12 receptor occupancy can be assessed using flow cytometry with P2Y12-specific antibodies or fluorescent ADP analogs. These assays confirm the compound's antiplatelet potency.
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| Animal Protocol |
In vivo animal studies for Elinogrel utilize models of arterial thrombosis, such as the ferric chloride-induced carotid artery thrombosis model or the Folts model of cyclic flow reductions. The compound is administered orally or intravenously. Endpoints include time to occlusion, thrombus weight, bleeding time, and ex vivo platelet aggregation. Efficacy is compared to vehicle and reference P2Y12 inhibitors (e.g., clopidogrel, ticagrelor). Pharmacodynamic assessments measure platelet inhibition over time.
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| ADME/Pharmacokinetics |
Elinogrel is orally and intravenously bioavailable. As a small molecule with molecular weight of 523.95 g/mol, it is soluble in DMSO at up to 100 mM. The compound's pharmacokinetic properties support both intravenous and oral administration, allowing flexibility for acute and chronic use. It is a direct-acting antagonist that does not require metabolic activation, unlike clopidogrel. Detailed PK parameters (half-life, Cmax, AUC, bioavailability) have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
In clinical trials, Elinogrel has been evaluated for safety and efficacy in ACS and PCI patients. Common adverse effects include bleeding (due to antiplatelet activity), dyspnea, and gastrointestinal symptoms. The compound's reversible binding may result in faster recovery of platelet function after drug discontinuation compared to irreversible agents. However, development may have been limited by bleeding risk or other safety concerns. Standard toxicology studies would have been conducted for IND-enabling development.
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| References |
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| Additional Infomation |
P2Y12 receptor inhibitor and platelet aggregation inhibitor.
Drug indications Investigations are underway for the treatment of cardiovascular disease and myocardial infarction.Mechanism of action PRT060128 is a specific, reversible ADP receptor antagonist that binds to the P2Y12 receptor on platelets. PRT060128 prevents adenosine diphosphate (ADP) from binding to its platelet receptor, thereby inhibiting ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, a key step in the coagulation cascade. The mechanism of action of PRT060128 may be similar to that of clopidogrel. Drug indications Investigations are underway for the treatment of cardiovascular disease and myocardial infarction. Elinogrel (PRT060128) is a potent, direct-acting, competitive, and reversible P2Y12 antagonist with IC50 of 20 nM. It has oral and intravenous bioavailability and potent antiplatelet effects. It was investigated for ACS and PCI. Unlike clopidogrel, it does not require metabolic activation. It is available for research purposes only. |
| Molecular Formula |
C20H15CLFN5O5S2
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|---|---|
| Molecular Weight |
523.95
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| Exact Mass |
523.018
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| Elemental Analysis |
C, 45.85; H, 2.89; Cl, 6.77; F, 3.63; N, 13.37; O, 15.27; S, 12.24
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| CAS # |
936500-94-6
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| Related CAS # |
936501-01-8 (potassium);936500-94-6;
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| PubChem CID |
16066663
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.706
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| LogP |
3.02
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
914
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NS(C1=CC=C(Cl)S1)(=O)=O)NC1C=CC(N2C(=O)C3C(=CC(=C(C=3)F)NC)NC2=O)=CC=1
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| InChi Key |
LGSDFTPAICUONK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15ClFN5O5S2/c1-23-15-9-14-12(8-13(15)22)18(28)27(20(30)25-14)11-4-2-10(3-5-11)24-19(29)26-34(31,32)17-7-6-16(21)33-17/h2-9,23H,1H3,(H,25,30)(H2,24,26,29)
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| Chemical Name |
1-(5-chlorothiophen-2-yl)sulfonyl-3-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1H-quinazolin-3-yl]phenyl]urea
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| Synonyms |
PRT 060128; PRT-060128; PRT060128; Elinogrel
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~119.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9086 mL | 9.5429 mL | 19.0858 mL | |
| 5 mM | 0.3817 mL | 1.9086 mL | 3.8172 mL | |
| 10 mM | 0.1909 mL | 0.9543 mL | 1.9086 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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