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Purity: ≥98%
Clopidogrel sulfate (Plavix; Zyllt; Osvix; Plavitor, SR-25990C), the sulfate salt of Clopidogrel, is an orally bioavailable, thienopyridine class of antiplatelet agent acting as an irreversible inhibitor of ADP receptor (P2Y12). Clopidogrel is a prodrug that has to be activated by CYP2C19. It is approved as an antiplatelet and anticoagulant medication used to reduce the risk of heart disease and stroke in those at high risk. Clopidogrel works by irreversibly inhibiting a receptor called P2Y12, an adenosine diphosphate (ADP) chemoreceptor on platelet cell membranes. Clopidogrel acts by inhibiting the ADP receptor on platelet cell membranes.
| ln Vitro |
According to real-time PCR and other methods, clopidogrel hydrogen sulfate (1.5 mM; 12 and 24 hours) increases the expression of TRIB3 and CHOP in a concentration- and time-dependent way.
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| ln Vivo |
When compared to a carrier, clopidogrel hydrogen sulfate (5 mg/kg) effectively prevented thrombosis. In mice, acetylsalicylic acid (0.15 mg/kg) can enhance clopidogrel's antithrombotic efficacy; in mice, acetylsalicylic acid (0.6 mg/kg) can reduce clopidogrel's antithrombotic effect [4].
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: GES-1 cells Tested Concentrations: 1.5 mM Incubation Duration: 12 and 24 hrs (hours) Experimental Results: The mRNA expression levels of both CHOP and TRIB3 were up-regulated in a concentration- and time-dependent manner. The protein expression levels of both CHOP and TRIB3 were up-regulated in a concentration- and time-dependent manner. Apoptosis Analysis[3] Cell Types: Gastric epithelial cell (GES-1) cells Tested Concentrations: 1.5 mM Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis of gastric epithelial cells． |
| Animal Protocol |
Animal/Disease Models: Age-matched C57BL/6J male mice weighing at least 25 g were used at 8 to 12 weeks of age[4]
Doses: 5 mg/kg Route of Administration: Gavage treatment Experimental Results: Clopidogrel Dramatically inhibited thrombus formation compared with vehicle. When Clopidogrel was given in combination with 0.6 mg/kg ASA, thrombi were Dramatically larger than those measured with Clopidogrel alone. In contrast, when Clopidogrel was given in combination with 0.15 mg/kg ASA, thrombi were Dramatically smaller than those in mice treated with Clopidogrel and 0.6 mg/kg ASA, and smaller than those in mice given Clopidogrel alone. |
| References |
[1]. Katsunobu Hagihara, et al. Comparison of human cytochrome P450 inhibition by the thienopyridines prasugrel, Clopidogrel, and ticlopidine. Drug Metab Pharmacokinet. 2008;23(6):412-20.
[2]. Jean-Marc Herbert, et al. P2Y12, a new platelet ADP receptor, target of Clopidogrel.Semin Vasc Med. 2003 May;3(2):113-22. [3]. Hai-Lu Wu, et al. Increased endoplasmic reticulum stress response is involved in Clopidogrel-induced apoptosis of gastric epithelial cells. PLoS One. 2013 Sep 13;8(9):e74381. [4]. Ran Ni, et al. Effect of Different Doses of Acetylsalicylic Acid on the Antithrombotic Activity of Clopidogrel in a Mouse Arterial Thrombosis Model.Arterioscler Thromb Vasc Biol. 2018 Oct;38(10):2338-2344. [5]. Kuszynski DS, et al. Clopidogrel treatment inhibits P2Y2-Mediated constriction in the rabbit middle cerebral artery [published online ahead of print, 2021 Oct 1]. Eur J Pharmacol. 2021;174545. |
| Molecular Formula |
C16H16CLNO2S.H2SO4
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| Molecular Weight |
419.9
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| CAS # |
120202-66-6
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| Related CAS # |
Clopidogrel;113665-84-2;Clopidogrel thiolactone;1147350-75-1;Clopidogrel-d3 hydrogen sulfate;1217643-68-9
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| SMILES |
ClC1=C([C@@H](C(OC)=O)N2CCC3=C(C=CS3)C2)C=CC=C1.O=S(O)(O)=O
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| InChi Key |
FDEODCTUSIWGLK-RSAXXLAASA-N
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| InChi Code |
InChI=1S/C16H16ClNO2S.H2O4S/c1-20-16(19)15(12-4-2-3-5-13(12)17)18-8-6-14-11(10-18)7-9-21-14;1-5(2,3)4/h2-5,7,9,15H,6,8,10H2,1H3;(H2,1,2,3,4)/t15-;/m0./s1
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| Chemical Name |
methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate sulfate
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| Synonyms |
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3815 mL | 11.9076 mL | 23.8152 mL | |
| 5 mM | 0.4763 mL | 2.3815 mL | 4.7630 mL | |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3815 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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