| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
Purity: ≥98%
| Targets |
P2Y12 receptor (ADP receptor on platelet membranes). Clopidogrel is a prodrug that is converted to its active metabolite by cytochrome P450 (CYP) enzymes. The active metabolite irreversibly inhibits the P2Y12 receptor on platelet membranes, blocking ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. This prevents platelet aggregation and thrombus formation.
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| ln Vitro |
Clopidogrel is converted to its active metabolite by cytochrome P450
(CYP) enzymes. Clopidogrel (1 μM) also inhibits EGF-stimulated EGF
receptor, PERK expression, and cell proliferation in RGM-1 cells
(P<0.05), and causes much less inhibition of EGF-stimulated cell
proliferation in EGF receptor over-expressed RGM-1 cells than in RGM-1
cells (22% vs. 32% reduction). Clopidogrel increases blood vessel
number, reduces polymorphonuclear count and decreases attachment and
bone loss, also decreases osteoclast number in rats submitted or not to
periodontal repair. Clopidogrel decreases CXCL4, CXCL12 and PDGF content
compared with saline-treated rats, without affecting CXCL5.
Clopidogrel sulfate is converted to its active metabolite by cytochrome P450 enzymes in vitro. The active metabolite inhibits ADP-induced platelet aggregation in a concentration-dependent manner. The compound's antiplatelet activity has been characterized in various in vitro assays using platelet-rich plasma or whole blood. |
| ln Vivo |
Clopidogrel
(2mg and 10mg/kg/day) significantly decreases ulcer-induced gastric
epithelial cell proliferation and ulcer-stimulated expressions of EGF
receptor and phosphorylated extracellular signal-regulated kinase (PERK)
at the ulcer margin of rats. Clopidogrel improves endothelial function
and NO bioavailability in rats with congestive heart failure.
Clopidogrel-treated Congestive heart failure (CHF) rat displays enhances
phosphorylation of AKT and eNOS. The clopidogrel/aspirin combination
shows only additive-type effects on bleeding time prolongation induced
by ear transection in the rabbit, therefore showing that combined
inhibition of cyclooxygenase and ADPs effects provide a marked enhanced
antithrombotic efficacy. |
| Enzyme Assay |
In vitro platelet aggregation assays for Clopidogrel sulfate involve using platelet-rich plasma or whole blood. The compound is incubated with platelets, and ADP-induced aggregation is measured using a platelet aggregometer. IC50 values are determined from dose-response curves. For active metabolite studies, Clopidogrel is incubated with liver microsomes or hepatocytes to generate the active metabolite, which is then tested in platelet aggregation assays.
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| Cell Assay |
Cellular assays for Clopidogrel sulfate are not typically performed, as the compound acts on platelets rather than on cultured cells. However, platelet function can be assessed in whole blood or platelet-rich plasma treated with Clopidogrel. P2Y12 receptor occupancy can be measured using flow cytometry with specific antibodies or by measuring VASP phosphorylation.
|
| Animal Protocol |
2mg and 10mg/kg | Rats
| ADME/Pharmacokinetics |
Clopidogrel sulfate is orally bioavailable and is absorbed from the gastrointestinal tract. It is a prodrug that is converted to its active metabolite by CYP enzymes in the liver. The compound has a molecular weight of 419.9 g/mol and a molecular formula of C16H18ClNO6S2. It is soluble in DMSO and should be stored at room temperature. Its elimination half-life is approximately 6-8 hours in humans.
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| Toxicity/Toxicokinetics |
Clopidogrel sulfate is generally well-tolerated but can cause bleeding complications, gastrointestinal disturbances, and hypersensitivity reactions. It is contraindicated in patients with active bleeding or severe liver impairment. The compound is an FDA-approved medication and is available as a prescription drug. It is also known by the brand name Plavix.
|
| References |
Eur J Pharmacol.2012 Nov 15;695(1-3):112-9;Basic Res Cardiol.2011 May;106(3):485-94. |
| Additional Infomation |
See also: Clopidogrel benzenesulfonate (note moved to).
Clopidogrel Sulfate (racemic) is a potent, orally bioavailable thienopyridine antiplatelet agent that irreversibly inhibits the P2Y12 receptor. It is approved for the prevention of thrombotic events in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. The compound is an FDA-approved medication and is available as a prescription drug. |
| Molecular Formula |
C16H18CLNO6S2
|
|---|---|
| Molecular Weight |
419.90022
|
| Exact Mass |
419.026
|
| CAS # |
135046-48-9
|
| Related CAS # |
(Rac)-Clopidogrel-d3 sulfate;2468372-74-7;Clopidogrel-d4 sulfate;1219274-96-0
|
| PubChem CID |
16757820
|
| Appearance |
Off-white to yellow solid powder
|
| Boiling Point |
423.7ºC at 760 mmHg
|
| Melting Point |
184ºC
|
| Flash Point |
210ºC
|
| Vapour Pressure |
8.71E-09mmHg at 25°C
|
| LogP |
4.039
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
463
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC(=O)C(C1=CC=CC=C1Cl)N2CCC3=C(C=CS3)C2.OS(=O)(=O)O
|
| InChi Key |
FDEODCTUSIWGLK-UHFFFAOYSA-N
|
| 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)7-9-21-141-5(2,3)4/h2-5,7,9,15H,6,8,10H2,1H3(H2,1,2,3,4)
|
| Chemical Name |
methyl 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetate sulfate
|
| Synonyms |
Clopidogrel hydrogen sulfate Myogrel SR 25990C SR-25990C SR-25990C
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00862420 | Completed | Drug: clopidogrel (SR25990) Drug: ticlopidine |
Peripheral Arterial Disease (PAD) | Sanofi | February 2009 | Phase 3 |
| NCT00821834 | Completed | Drug: clopidogrel (SR25990) Drug: ticlopidine |
Stable Angina Myocardial Infarction |
Sanofi | December 2008 | Phase 3 |
| NCT00386191 | Completed | Drug: clopidogrel (SR25990C) | Cerebral Infarction | Sanofi | September 2006 | Phase 4 |
| NCT01400035 | Completed | Cerebral Infarction | Shanghai Rxmidas Pharmaceuticals Co. Ltd. |
May 2010 |
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