| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
Vicagrel targets the P2Y12 receptor, a G-protein-coupled receptor on platelets that mediates ADP-induced platelet aggregation. By irreversibly inhibiting the P2Y12 receptor, it blocks platelet activation and aggregation, thereby exerting its antiplatelet effects. It is a substrate of carboxylesterase 2 (CES2).
|
|---|---|
| ln Vitro |
Vicagrel (compound 9a) (20 μM, 30 min) stimulates the in vitro rat liver microsomal production of the active metabolite[1].
In vitro, vicagrel acts as a potent P2Y12 receptor inhibitor. As an acetate derivative of clopidogrel, it is designed to have improved metabolic activation properties. It reduces metabolic inactivation and enhances the inhibitory effect of aspirin on platelet aggregation and thrombosis in rodents. |
| ln Vivo |
Vicagrel (compound 9a) (oral, 3 mg/kg) inhibits the aggregation of platelets in rats induced by ADP[1].
Vicagrel (orally, 1.14 mg/mL, 0–24 h) has a low clinically effective dose, good bioavailability, and good preliminary pharmacokinetics[1]. Vicagrel (oral, 5 g/kg, single, for 14 days) exhibits minimal dose-related toxicity in mouse[1]. In vivo, vicagrel has shown efficacy in rodent models by reducing metabolic inactivation and enhancing the inhibitory effect of aspirin on platelet aggregation and thrombosis. It is an orally active antiplatelet agent. It has been investigated for the treatment of coronary artery disease. Detailed in vivo efficacy data are not provided. |
| Enzyme Assay |
P2Y12 receptor binding affinity is determined using radioligand binding assays with membrane preparations from platelets or cells expressing the P2Y12 receptor. Competitive displacement of a labeled P2Y12-specific ligand is measured, and binding parameters are calculated. Platelet aggregation assays are used to assess functional inhibition.
|
| Cell Assay |
Cellular assays for vicagrel use platelet aggregation assays. Platelet-rich plasma is treated with the compound, and ADP-induced platelet aggregation is measured using aggregometry. Inhibition of aggregation indicates P2Y12 receptor antagonism. The compound's effects on platelet function are evaluated ex vivo in animal models.
|
| Animal Protocol |
Male Wistar rats, (200−250 g)
3 mg/kg oral In vivo animal studies for vicagrel are conducted in rodent models of thrombosis and platelet aggregation. The compound is administered orally, and platelet aggregation is measured ex vivo. Efficacy in inhibiting thrombosis is assessed in appropriate models. The compound's ability to enhance aspirin's antiplatelet effects is also evaluated. |
| ADME/Pharmacokinetics |
Vicagrel has the molecular formula C₁₈H₁₈ClNO₄S with a molecular weight of 379.86. It is orally active. It is an acetate derivative of clopidogrel and a substrate of carboxylesterase 2 (CES2). Detailed pharmacokinetic parameters are not disclosed.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are detailed in the available references. The compound is described as a "safe" antiplatelet agent. As a P2Y12 inhibitor, potential toxicities may include bleeding risk, which is a class effect of antiplatelet agents. Its improved metabolic profile may offer a favorable safety margin.
|
| References | |
| Additional Infomation |
Vicagrel is being studied in the clinical trial NCT03599284 (Efficacy, safety and pharmacokinetics of Vicagrel antiplatelet therapy).
Vicagrel is an investigational compound not yet approved for clinical use. It is an acetate derivative of clopidogrel designed as a P2Y12 platelet inhibitor for the treatment of thrombosis. Its potential advantages include reduced metabolic inactivation and enhanced antiplatelet effects when combined with aspirin. It has been studied for the treatment of coronary artery disease. |
| Molecular Formula |
C18H18CLNO4S
|
|
|---|---|---|
| Molecular Weight |
379.86
|
|
| Exact Mass |
379.065
|
|
| Elemental Analysis |
C, 56.92; H, 4.78; Cl, 9.33; N, 3.69; O, 16.85; S, 8.44
|
|
| CAS # |
1314081-53-2
|
|
| Related CAS # |
|
|
| PubChem CID |
53378151
|
|
| Appearance |
White to off-white solid powder
|
|
| LogP |
3.537
|
|
| Hydrogen Bond Donor Count |
0
|
|
| Hydrogen Bond Acceptor Count |
6
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
25
|
|
| Complexity |
506
|
|
| Defined Atom Stereocenter Count |
1
|
|
| SMILES |
ClC1C=CC=CC=1[C@@H](C(=O)OC)N1CC2C=C(OC(C)=O)SC=2CC1
|
|
| InChi Key |
GNHHCBSBCDGWND-KRWDZBQOSA-N
|
|
| InChi Code |
InChI=1S/C18H18ClNO4S/c1-11(21)24-16-9-12-10-20(8-7-15(12)25-16)17(18(22)23-2)13-5-3-4-6-14(13)19/h3-6,9,17H,7-8,10H2,1-2H3/t17-/m0/s1
|
|
| Chemical Name |
methyl (2S)-2-(2-acetyloxy-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)-2-(2-chlorophenyl)acetate
|
|
| Synonyms |
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6325 mL | 13.1627 mL | 26.3255 mL | |
| 5 mM | 0.5265 mL | 2.6325 mL | 5.2651 mL | |
| 10 mM | 0.2633 mL | 1.3163 mL | 2.6325 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 |
| NCT05651074 | Recruiting | Drug: Vicagrel and omeprazole | Healthy Subjects | Jiangsu vcare pharmaceutical technology co., LTD |
November 14, 2022 | Phase 1 |
| NCT04143750 | Completed | Drug: [14C]Vicagrel | Healthy Male Adult | Jiangsu vcare pharmaceutical technology co., LTD |
November 11, 2019 | Phase 1 |
| NCT05162053 | Completed | Drug: vicagrel Capsules Drug: Clopidogrel Tablets |
Acute Coronary Syndrome | Jiangsu vcare pharmaceutical technology co., LTD |
December 9, 2021 | Phase 1 |
| NCT04919551 | Completed | Drug: vicagrel | Acute Coronary Syndrome | Jiangsu vcare pharmaceutical technology co., LTD |
August 24, 2021 | Phase 1 |
| NCT03599284 | Completed | Drug: Vicagrel 5mg Drug: Vicagrel 6mg |
Coronary Artery Disease Platelet Aggregation Inhibitors |
Jiangsu vcare pharmaceutical technology co., LTD |
August 30, 2018 | Phase 2 |
J Med Chem.2012 Apr 12;55(7):3342-52. |
|---|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
