Vicagrel
Based on 1 publication(s) in Google Scholar
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 1314081-53-2
- 分子式: C18H18ClNO4S
- 分子量:379.86
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Vicagrel
MoreP2Y Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
体外実験
Vicagrel (compound 9a) (20 μM, 30 min) activates production of the active metabolite from in vitro rat liver microsomal[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Vicagrel (oral, 1.14 mg/mL, 0-24 h) has giood preliminary pharmacokinetic with high bioavailability and low clinically effective dose[1].
Vicagrel (oral, 5 g/kg, single, for 14 days) has low dose-related toxicity in mouse[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[1]
(200−250 g) -
Dosage:3 mg/kg
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Administration:oral
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Result:Inhibitied platelet aggregation by ADP-induced in rats.
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Animal Model:SD male rats[1]
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Dosage:1.14 mg/mL
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Administration:oral, 0-24 h
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Result:Could be readily converted into clopidogrel thiolactone and had high bioavailability.
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Animal Model:Mice[1]
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Dosage:5 g/kg
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Administration:oral, single, for 14 days
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Result:Had very low acute toxicity.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1314081-53-2
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性状 Solid
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分子量 379.86
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分子式 C18H18ClNO4S
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Color White to off-white
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SMILES
O=C(OC)[C@@H](N1CCC2=C(C=C(OC(C)=O)S2)C1)C3=CC=CC=C3Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Chem Biol Interact
Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions. [Abstract]2022 Jan 25:352:109775. PMID: 34910929
溶剤 & 溶解度
体外:
DMSO : 250 mg/mL (658.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
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- Italian - IT (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6325 mL | 13.1627 mL | 26.3255 mL | 65.8137 mL |
| 5 mM | 0.5265 mL | 2.6325 mL | 5.2651 mL | 13.1627 mL | |
| 10 mM | 0.2633 mL | 1.3163 mL | 2.6325 mL | 6.5814 mL | |
| 15 mM | 0.1755 mL | 0.8775 mL | 1.7550 mL | 4.3876 mL | |
| 20 mM | 0.1316 mL | 0.6581 mL | 1.3163 mL | 3.2907 mL | |
| 25 mM | 0.1053 mL | 0.5265 mL | 1.0530 mL | 2.6325 mL | |
| 30 mM | 0.0878 mL | 0.4388 mL | 0.8775 mL | 2.1938 mL | |
| 40 mM | 0.0658 mL | 0.3291 mL | 0.6581 mL | 1.6453 mL | |
| 50 mM | 0.0527 mL | 0.2633 mL | 0.5265 mL | 1.3163 mL | |
| 60 mM | 0.0439 mL | 0.2194 mL | 0.4388 mL | 1.0969 mL | |
| 80 mM | 0.0329 mL | 0.1645 mL | 0.3291 mL | 0.8227 mL | |
| 100 mM | 0.0263 mL | 0.1316 mL | 0.2633 mL | 0.6581 mL |