Clopidogrel hydrogen sulfate (Synonyms: SR 25990C) |
رقم الكتالوجGC15964
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120202-66-6
Sample solution is provided at 25 µL, 10mM.
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Clopidogrel hydrogen sulfate is an orally effective purine-type P2Y12 receptor antagonist. The IC50 values for cytochrome P450 (CYP) subtypes CYP2B6 and CYP2C19 are 18.2nM and 524nM, respectively [1-2]. The P2Y12 receptor combines with the Gq pathway and promotes the release of intracellular calcium ions, thereby regulating the shape changes and aggregation process of platelets [3]. Clopidogrel hydrogen sulfate is a potent antithrombotic drug that can inhibit platelet aggregation triggered by adenosine diphosphate (ADP) [4].
In vitro, Clopidogrel hydrogen sulfate (0.5, 1.5mM; 24, 48h) upregulated the mRNA expression levels of TRIB3 and CHOP in GES-1 cells in a concentration- and time-dependent manner [5]. Clopidogrel hydrogen sulfate (1, 10 and 100μM; 24h) treatment concentration-dependently increased the cytotoxicity and intracellular ROS levels of HepG2 cells (expressing human CYP3A4) [6].
In the body, Clopidogrel hydrogen sulfate (1.25, 2.5, 3.75 and 5mg/kg; twice; gavage) can significantly inhibit thrombosis formation in a dose-dependent manner in the mouse arterial thrombosis model. When combined with acetylsalicylic acid (0.15mg/kg), it can enhance the antithrombotic effect of Clopidogrel hydrogen sulfate, while acetylsalicylic acid (0.6mg/kg) can weaken its antithrombotic effect [7]. 24 hours before the ischemia-reperfusion surgery, oral administration of Clopidogrel hydrogen sulfate (25mg/kg/day) significantly reduced the plasma levels of blood urea nitrogen (BUN) and creatinine in mice with renal ischemia-reperfusion injury (IRI), increased the expression of Bcl-2 and Bcl-xL, caspase-3 and caspase-8, and decreased the number of CD41-positive cells [8].
References:
[1] Laine L, Hennekens C. Proton pump inhibitor and clopidogrel interaction: fact or fiction?. Am J Gastroenterol. 2010;105(1):34-41.
[2] 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.
[3] Dorsam R T, Murugappan S, Ding Z, et al. Clopidogrel: interactions with the P2Y12 receptor and clinical relevance[J]. Hematology, 2003, 8(6): 359-365.
[4] Herbert JM, Savi P. P2Y12, a new platelet ADP receptor, target of clopidogrel. Semin Vasc Med. 2003;3(2):113-122.
[5] Wu HL, Duan ZT, Jiang ZD, Cao WJ, Wang ZB, Hu KW, Gao X, Wang SK, He BS, Zhang ZY, Xie HG. Increased endoplasmic reticulum stress response is involved in clopidogrel-induced apoptosis of gastric epithelial cells. PLoS One. 2013 Sep 13;8(9):e74381.
[6] Zahno A, Bouitbir J, Maseneni S, Lindinger PW, Brecht K, Krähenbühl S. Hepatocellular toxicity of clopidogrel: mechanisms and risk factors. Free Radic Biol Med. 2013;65:208-216.
[7] Ni R, Vaezzadeh N, Zhou J, Weitz JI, Cattaneo M, Gross PL. 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.
[8] Hu H, Batteux F, Chéreau C, et al. Clopidogrel protects from cell apoptosis and oxidative damage in a mouse model of renal ischaemia–reperfusion injury[J]. The Journal of pathology, 2011, 225(2): 265-275.
| Cell experiment [1]: | |
Cell lines | GES-1 cells |
Preparation Method | GES-1 cells were plated in 60-mm dishes (3ml, 1×106/well) and incubated for 24h at 37°C. After 24-h treatment with Clopidogrel hydrogen sulfate, the cells were collected and washed twice with ice-cold PBS, and then were re-suspended in binding buffer at a concentration of 1×106 cells/ml and incubated with 10µl of PI (50µg/ml) solution and 5µl of FITC-conjugated AV (17.6µg/ml) at 37°C for 5min in the dark to achieve double staining. After staining, 400µl of binding buffer were added to the cells, and then analyzed by flow cytometry. |
Reaction Conditions | 1.5mM; 24h |
Applications | Clopidogrel hydrogen sulfate significantly inhibits the proliferation of GES-1 cells and induces apoptosis. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Clopidogrel hydrogen sulfate were dissolved in diluted apple jelly and acetylsalicylic acid (ASA) were dissolved in distilled water. Age-matched C57BL/6J male mice weighing at least 25g were used at 8 to 12 weeks of age. Anesthesia was initiated with an intraperitoneal injection of 125mg/kg of ketamine, 12.5mg/kg of xylazine, and 0.25mg/kg of atropine and maintained with Nembutal. All mice received 100μL of vehicle or an equal volume of ASA, Clopidogrel hydrogen sulfate or both by gavage using 20-gauge animal feeding needles. ASA was given only once, 4 hours before study, whereas clopidogrel was given twice: 24 and 4 hours before study. ASA and clopidogrel were given at doses up to 5mg/kg body weight. Blood samples were collected via carotid artery cannulation into 3.2% sodium citrate at a ratio of 9:1 (vol:vol). Blood was diluted and recalcified with 1.5mM CaCl2, and platelet aggregation, quantified by area under the curve (AUC), in whole blood was recorded for 6min after using a Multiplate Analyzer. |
Dosage form | 1.25, 2.5, 3.75, or 5mg/kg; twice; gavage |
Applications | Clopidogrel hydrogen sulfate can significantly inhibit thrombosis formation in a dose-dependent manner in a mouse model of arterial thrombosis. When used in combination with acetylsalicylic acid (0.15mg/kg), it can enhance the antithrombotic effect of Clopidogrel hydrogen sulfate, while acetylsalicylic acid (0.6mg/kg) will weaken its antithrombotic effect. |
References: | |
| Cas No. | 120202-66-6 | SDF | |
| المرادفات | SR 25990C | ||
| Chemical Name | methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate;sulfuric acid | ||
| Canonical SMILES | COC(=O)C(C1=CC=CC=C1Cl)N2CCC3=C(C2)C=CS3.OS(=O)(=O)O | ||
| Formula | C16H16ClNO2S.H2SO4 | M.Wt | 419.9 |
| الذوبان | ≥ 100mg/ml in DMSO, ≥ 50 mg/mL in EtOH with ultrasonic, ≥ 48.6 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3815 mL | 11.9076 mL | 23.8152 mL |
| 5 mM | 476.3 μL | 2.3815 mL | 4.763 mL |
| 10 mM | 238.2 μL | 1.1908 mL | 2.3815 mL |
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)