| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
P2Y1/P2Y12 antagonist-1 targets the P2Y1 and P2Y12 purinergic receptors, which are involved in platelet activation and aggregation. The compound is a dual inhibitor with antiplatelet activity. It inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. By inhibiting both receptors, the antagonist prevents blood clot formation and may reduce the risk of cardiovascular events. It also shows effects in rat thrombosis models.
|
|---|---|
| ln Vitro |
In vitro studies demonstrate that P2Y1/P2Y12 antagonist-1 is a dual inhibitor of P2Y1 and P2Y12 receptors with antiplatelet activity. It inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. This activity indicates potent inhibition of platelet activation pathways. The compound's ability to inhibit both P2Y1 and P2Y12 receptors provides comprehensive antiplatelet effects. Detailed receptor binding affinity data (Ki values) are not extensively documented.
|
| ln Vivo |
In vivo activity of P2Y1/P2Y12 antagonist-1 has been demonstrated in rat thrombosis models, where it shows potent inhibitory effects. As an orally available compound, it is suitable for convenient administration in research settings. By inhibiting platelet aggregation, the compound may prevent thrombus formation and reduce the risk of cardiovascular events such as stroke and myocardial infarction. Detailed in vivo efficacy data, including dose-response relationships and thrombus reduction, are not extensively documented.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for P2Y1/P2Y12 antagonist-1 typically involves measuring its ability to inhibit ADP-induced platelet aggregation. Platelet-rich plasma from rabbits is incubated with the compound at varying concentrations, followed by stimulation with ADP. Aggregation is measured using aggregometry, and the IC50 value is determined by plotting percentage inhibition against compound concentration. Receptor binding assays using radiolabeled ligands and membrane preparations may also be performed to determine binding affinities.
|
| Cell Assay |
In vitro cell-based assays for P2Y1/P2Y12 antagonist-1 are conducted using platelet-rich plasma or washed platelets. Platelets are treated with the compound at various concentrations, and aggregation is induced by ADP or other agonists. Aggregation is measured using light transmission aggregometry or impedance aggregometry. The compound's ability to inhibit platelet activation is assessed by measuring markers such as P-selectin expression or ATP release. Standard protocols include appropriate positive controls such as known P2Y12 inhibitors.
|
| Animal Protocol |
In vivo animal studies for P2Y1/P2Y12 antagonist-1 are conducted using rat thrombosis models. Animals are administered the compound orally, and thrombus formation is induced by methods such as ferric chloride injury or arteriovenous shunt. Antithrombotic efficacy is evaluated by measuring thrombus weight, occlusion time, or bleeding time. Pharmacokinetic parameters are determined from plasma samples. The compound's oral activity is evaluated by comparing efficacy following oral administration.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of P2Y1/P2Y12 antagonist-1 include oral availability, indicating good oral bioavailability. The compound is identified as compound 24w. Detailed pharmacokinetic parameters such as half-life, Cmax, and tissue distribution are not extensively documented in the available literature. The compound is intended for research use only. Storage and formulation details are not provided in the search results.
|
| Toxicity/Toxicokinetics |
Toxicity information for P2Y1/P2Y12 antagonist-1 is limited in the available literature. As an antiplatelet agent, potential bleeding risk should be considered. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
|
| References | |
| Additional Infomation |
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 receptors with antiplatelet activity. It inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. It may be useful in preventing blood clot formation and reducing the risk of cardiovascular events such as stroke and myocardial infarction. It shows potent inhibitory effects in rat thrombosis models.
|
| Molecular Formula |
C22H18N4O3
|
|---|---|
| Molecular Weight |
386.40
|
| Exact Mass |
386.137
|
| CAS # |
2738381-94-5
|
| PubChem CID |
162661404
|
| Appearance |
White to off-white solid powder
|
| LogP |
4
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
658
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC(=O)C1=C(N=C(N1OCC2=CC=C(C=C2)C#N)C3=CC=CC(=C3)C#N)C
|
| InChi Key |
AQVZLXOFKCFLKL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H18N4O3/c1-3-28-22(27)20-15(2)25-21(19-6-4-5-18(11-19)13-24)26(20)29-14-17-9-7-16(12-23)8-10-17/h4-11H,3,14H2,1-2H3
|
| Chemical Name |
ethyl 2-(3-cyanophenyl)-3-[(4-cyanophenyl)methoxy]-5-methylimidazole-4-carboxylate
|
| 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 |
| 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) |
DMSO :~2 mg/mL (~5.18 mM; with sonication (<60°C))
|
|---|---|
| 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 | 2.5880 mL | 12.9400 mL | 25.8799 mL | |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
