| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Clopidogrel thiolactone (also known as 2-Oxoclopidogrel) is a metabolite of Clopidogrel which is a P2Y12 receptor inhibitor. Clopidogrel's first oxidative activation produces clopidogrel thiolactone, a metabolic intermediate. Based on clopidogrel thiolactone modification, vicagrel's antiplatelet potency was significantly higher than clopidogrel's and comparable to prasugrel's. A significantly lower clinically effective dose for vicagrel in comparison to clopidogrel is implied by preliminary pharmacokinetic study results, which showed that the bioavailability of clopidogrel thiolactone generated from vicagrel was 6-fold higher than that generated from clopidogrel. Conclusion: Compared to clopidogrel, vicagrel appears to be a safer and more effective antiplatelet agent. It may also have the following benefits: (1) no drug resistance for CYP2C19 poor metabolizers; (2) lower dose-related toxicity because of a much lower effective dose; and (3) a faster onset of action.
| Targets |
P2Y12 Receptor
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|---|---|---|
| ln Vitro |
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| ln Vivo |
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| Animal Protocol |
Sprague-Dawley male rats
8 μm/kg; orally clopidogrel (24 μm/kg) Intravenous injection; collected blood at 0 h (before dosing) and 0.083, 0.167, 0.5, 1, 2, 4, 6, 8, 24 h postdose. |
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| References |
| Molecular Formula |
C16H16CLNO3S
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| Molecular Weight |
337.82
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| Exact Mass |
337.05
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| Elemental Analysis |
C, 56.89; H, 4.77; Cl, 10.49; N, 4.15; O, 14.21; S, 9.49
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| CAS # |
1147350-75-1
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| Related CAS # |
Clopidogrel; 113665-84-2; Clopidogrel hydrogen sulfate; 120202-66-6
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| Appearance |
Solid powder
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| SMILES |
COC(=O)[C@H](C1=CC=CC=C1Cl)N2CCC3C(=CC(=O)S3)C2
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| InChi Key |
JBSAZVIMJUOBNB-WUJWULDRSA-N
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| InChi Code |
InChI=1S/C16H16ClNO3S/c1-21-16(20)15(11-4-2-3-5-12(11)17)18-7-6-13-10(9-18)8-14(19)22-13/h2-5,8,13,15H,6-7,9H2,1H3/t13?,15-/m0/s1
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| Chemical Name |
methyl (2S)-2-(2-chlorophenyl)-2-(2-oxo-4,6,7,7a-tetrahydrothieno[3,2-c]pyridin-5-yl)acetate
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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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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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9602 mL | 14.8008 mL | 29.6016 mL | |
| 5 mM | 0.5920 mL | 2.9602 mL | 5.9203 mL | |
| 10 mM | 0.2960 mL | 1.4801 mL | 2.9602 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.
J Med Chem.2012 Apr 12;55(7):3342-52. |
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