Lacidipine
Based on 2 publication(s) in Google Scholar
Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
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: 99.40%
- CAS 番号: 103890-78-4
- 分子式: C26H33NO6
- 分子量:455.54
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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 Lacidipine
MoreCalcium Channel アイソフォーム固有の製品をすべて表示
MoreCaspase 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
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L-type calcium channel |
Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner[1].
Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HKC cells
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Concentration:0.01-100 μM
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Incubation Time:24 h
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Result:Exhibited anti-proliferative activity in a concentration-dependent manner.
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Cell Line:HKC cells (renal ischemia reperfusion (I/R) model)
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Concentration:1, 10 μM
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Incubation Time:24 h
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Result:AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively.
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Cell Line:HKC cells (renal ischemia reperfusion (I/R) model)
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Concentration:1, 10 μM
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Incubation Time:24 h (pretreat)
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Result:Decreased the expression of cyt c of injured cells following ATP depletion and recovery.
Significantly increased the expression of the Bcl-2 protein, but decreased the Bax protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 mice (Homozygous; apoE-deficient; atherosclerosis model)[2].
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Dosage:0.3, 1.0, 3.0 mg/kg
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Administration:Oral gavage; single daily for 10 weeks.
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Result:Induced a significant dose-dependent decrease in plasma endothelin levels.
Significantly reduced the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 103890-78-4
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性状 Solid
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分子量 455.54
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分子式 C26H33NO6
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Color White to off-white
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SMILES
O=C(C1=C(C)NC(C)=C(C(OCC)=O)C1C2=CC=CC=C2/C=C/C(OC(C)(C)C)=O)OCC
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別名
ラシジピン
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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 (2)
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Journal Impact Factor
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Most Recent
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Sci Rep
Elucidating host cell response pathways and repurposing therapeutics for SARS-CoV-2 and other coronaviruses. [Abstract]2022 Nov 5;12(1):18811. PMID: 36335206 -
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (109.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (279 KB)
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SDS (392 KB)
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- Portuguese - PT (392 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 | 2.1952 mL | 10.9760 mL | 21.9520 mL | 54.8799 mL |
| 5 mM | 0.4390 mL | 2.1952 mL | 4.3904 mL | 10.9760 mL | |
| 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL | 5.4880 mL | |
| 15 mM | 0.1463 mL | 0.7317 mL | 1.4635 mL | 3.6587 mL | |
| 20 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7440 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8781 mL | 2.1952 mL | |
| 30 mM | 0.0732 mL | 0.3659 mL | 0.7317 mL | 1.8293 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3720 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0976 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3659 mL | 0.9147 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6860 mL | |
| 100 mM | 0.0220 mL | 0.1098 mL | 0.2195 mL | 0.5488 mL |