Elinogrel
Based on 1 Customer Validation
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects.
For research use only. We do not sell to patients.
- Purity: 98.29%
- CAS No.: 936500-94-6
- Formula: C20H15ClFN5O5S2
- Molecular Weight:523.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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P2Y12 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
10 μM
Compound: 63
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Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation
Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation
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[PMID: 34731765] |
| Platelet | IC50 |
2.81 μM
Compound: 2, PRT-128
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Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method
Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method
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[PMID: 22984835] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 936500-94-6
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Appearance Solid
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Molecular Weight 523.95
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Formula C20H15ClFN5O5S2
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Color White to off-white
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SMILES
O=S(C1=CC=C(Cl)S1)(NC(NC2=CC=C(N3C(NC4=C(C=C(F)C(NC)=C4)C3=O)=O)C=C2)=O)=O
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Synonyms
PRT060128
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (119.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Angiolillo DJ, et al. Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudyfrom the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (INNOVATE-PCI) trial. Circ Cardiovasc Interv. 2012 Jun;5(3):347-56. [Content Brief]
[2]. Jacobson KA, et al. Pharmacochemistry of the platelet purinergic receptors. Purinergic Signal. 2011 Sep;7(3):305-24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9086 mL | 9.5429 mL | 19.0858 mL | 47.7145 mL |
| 5 mM | 0.3817 mL | 1.9086 mL | 3.8172 mL | 9.5429 mL | |
| 10 mM | 0.1909 mL | 0.9543 mL | 1.9086 mL | 4.7714 mL | |
| 15 mM | 0.1272 mL | 0.6362 mL | 1.2724 mL | 3.1810 mL | |
| 20 mM | 0.0954 mL | 0.4771 mL | 0.9543 mL | 2.3857 mL | |
| 25 mM | 0.0763 mL | 0.3817 mL | 0.7634 mL | 1.9086 mL | |
| 30 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5905 mL | |
| 40 mM | 0.0477 mL | 0.2386 mL | 0.4771 mL | 1.1929 mL | |
| 50 mM | 0.0382 mL | 0.1909 mL | 0.3817 mL | 0.9543 mL | |
| 60 mM | 0.0318 mL | 0.1590 mL | 0.3181 mL | 0.7952 mL | |
| 80 mM | 0.0239 mL | 0.1193 mL | 0.2386 mL | 0.5964 mL | |
| 100 mM | 0.0191 mL | 0.0954 mL | 0.1909 mL | 0.4771 mL |
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