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| Targets |
Cyclooxygenase (COX). Pamicogrel is a potent and selective inhibitor of cyclooxygenase (COX) with significant antiplatelet activity. COX is an enzyme that catalyzes the conversion of arachidonic acid to prostaglandins and thromboxanes, which are mediators of inflammation, pain, and platelet aggregation. By inhibiting COX, Pamicogrel reduces the production of thromboxane A2, a potent platelet aggregator and vasoconstrictor, thereby inhibiting platelet aggregation and thrombus formation. The compound's antiplatelet activity makes it a potential candidate for the prevention and treatment of thromboembolic disorders, including acute coronary syndrome and stroke. Pamicogrel is also known as KBT-3022. The compound's mechanism of action is well-defined and centered on the inhibition of COX, similar to other antiplatelet agents such as aspirin. However, Pamicogrel's selectivity and potency may offer advantages over existing therapies.
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| ln Vitro |
Pamidogrel is a cyclooxygenase inhibitor that Kanebo is developing to treat chronic arterial occlusion. It has antiplatelet aggregation characteristics. Additionally, ischemic brain injury may be prevented and treated with napidogrel [1].
Pamicogrel is a potent and selective COX inhibitor with significant antiplatelet activity. The compound inhibits platelet aggregation in vitro, as demonstrated in platelet-rich plasma assays. By inhibiting COX, Pamicogrel reduces the production of thromboxane A2, a potent platelet aggregator, thereby inhibiting platelet aggregation. The compound's antiplatelet activity has been characterized in various in vitro assays, including aggregation induced by arachidonic acid, collagen, and ADP. Pamicogrel's potency and selectivity for COX over other enzymes contribute to its specificity and reduced off-target effects. The compound's mechanism of action is similar to that of other antiplatelet agents, but its distinct chemical structure may offer advantages in terms of potency, selectivity, or pharmacokinetics. |
| ln Vivo |
Pamicogrel has been extensively studied in vivo for its antiplatelet and antithrombotic effects. The compound inhibits platelet aggregation and thrombus formation in animal models of thrombosis. By reducing thromboxane A2 production, Pamicogrel prevents platelet activation and aggregation, reducing the risk of thromboembolic events. The compound has been evaluated for its potential therapeutic applications in cardiovascular diseases, such as acute coronary syndrome and stroke. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical studies. Pamicogrel is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
COX enzyme inhibition assays are performed using recombinant COX-1 and COX-2 enzymes. The enzyme is incubated with the substrate arachidonic acid and a peroxidase co-substrate in assay buffer. The reaction product prostaglandin G2 is detected by measuring the oxidation of a chromogenic co-substrate (e.g., TMPD) at 590 nm. Pamicogrel is serially diluted in DMSO and added to the reaction mixture to determine IC50 values. Platelet aggregation assays are performed using platelet-rich plasma (PRP) prepared from human or animal blood. Aggregation is induced by agonists such as arachidonic acid, collagen, or ADP, and the extent of aggregation is measured using an aggregometer. Each concentration is tested in duplicate, and IC50 values are calculated by non-linear regression analysis. Appropriate positive controls (e.g., aspirin, indomethacin) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cellular COX inhibition and antiplatelet activity are evaluated in platelets and other cell types. Platelets are isolated from whole blood and treated with Pamicogrel at various concentrations. COX activity in platelets is assessed by measuring thromboxane B2 (a stable metabolite of thromboxane A2) production by ELISA. Platelet aggregation is assessed using aggregometry. Cell viability is assessed using MTT or LDH assays. Each experiment includes vehicle controls (DMSO) and appropriate positive controls (e.g., aspirin).
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| Animal Protocol |
In vivo efficacy of Pamicogrel is evaluated in animal models of thrombosis and cardiovascular disease. The compound is administered orally or intravenously at doses determined by preclinical studies. In models of arterial thrombosis, the compound's ability to prevent thrombus formation is assessed. In models of stroke, the compound's effects on infarct size and neurological outcome are evaluated. Platelet aggregation and thromboxane B2 levels are measured ex vivo. Pharmacokinetic parameters are assessed in parallel. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 448.53. Formula: C25H24N2O4S. CAS No.: 101001-34-7. IUPAC Name: 2-[4,5-Bis(4-methoxyphenyl)-2-thiazolyl]-1H-pyrrole-1-acetic acid ethyl ester. Synonyms: Pamicogrel; KBT-3022. Appearance: Solid. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Powder at -20°C for up to 3 years; 4°C for up to 2 years; In solvent at -80°C for up to 6 months; -20°C for up to 1 month. Pamicogrel is a potent and selective COX inhibitor with significant antiplatelet activity.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Pamicogrel. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a COX inhibitor, potential toxicities may include gastrointestinal ulceration and bleeding, similar to other NSAIDs. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References |
[1]. Light P. Pamicogrel (Kanebo). IDrugs. 1999 Sep;2(9):938-42.
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| Additional Infomation |
Pamicogrel is also known as KBT-3022. Its IUPAC name is 2-[4,5-Bis(4-methoxyphenyl)-2-thiazolyl]-1H-pyrrole-1-acetic acid ethyl ester. Pamicogrel is a potent and selective inhibitor of cyclooxygenase (COX) with significant antiplatelet activity. It belongs to the class of thienopyridine antiplatelet agents and has been extensively studied for its potential therapeutic applications in cardiovascular diseases, such as acute coronary syndrome and stroke. By inhibiting COX, Pamicogrel reduces thromboxane A2 production, inhibiting platelet aggregation and thrombus formation. No clinical trials have been reported for this compound. Pamicogrel is for research use only.
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| Molecular Formula |
C25H24N2O4S
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| Molecular Weight |
448.53406
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| Exact Mass |
448.146
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| CAS # |
101001-34-7
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| PubChem CID |
65870
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.22g/cm3
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| Boiling Point |
600.3ºC at 760mmHg
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| Flash Point |
316.8ºC
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| Vapour Pressure |
2.28E-14mmHg at 25°C
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| Index of Refraction |
1.612
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| LogP |
5.525
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
593
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(OCC)CN1C(C2=NC(C3=CC=C(OC)C=C3)=C(C4=CC=C(OC)C=C4)S2)=CC=C1
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| InChi Key |
ISCHOARKJADAKJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24N2O4S/c1-4-31-22(28)16-27-15-5-6-21(27)25-26-23(17-7-11-19(29-2)12-8-17)24(32-25)18-9-13-20(30-3)14-10-18/h5-15H,4,16H2,1-3H3
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| Chemical Name |
ethyl 2-[2-[4,5-bis(4-methoxyphenyl)-1,3-thiazol-2-yl]pyrrol-1-yl]acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~83.33 mg/mL (~185.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2295 mL | 11.1475 mL | 22.2951 mL | |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.4590 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2295 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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