Efonidipine
Based on 1 publication(s) in Google Scholar
Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis.
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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: 99.88%
- CAS 番号: 111011-63-3
- 分子式: C34H38N3O7P
- 分子量:631.66
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Efonidipine
MoreCalcium Channel 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 1.8 nM (IC50) |
T-type calcium channel 350 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LLC-PK1 | IC50 |
13 μM
Compound: Efonidipine
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 12128170] |
| LLC-PK1 | IC50 |
17.3 μM
Compound: Efonidipine
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TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (-)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (-)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 11145223] |
| LLC-PK1 | IC50 |
20.6 μM
Compound: Efonidipine
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TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (+)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (+)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 11145223] |
Efonidipine (10 μM, 24 h) induces an increase in StAR mRNA that is independent of extracellular Ca2+ in NCI-H295R human adrenocortical cells[2].
Efonidipine (1 μM, 24 h) significantly increases the production of DHEA-S in NCI-H295R human adrenocortical cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H295R human adrenocortical cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Dose-dependently and significantly enhanced the dbcAMP-induced expression of StAR mRNA.
Enhanced the angiotensin II-induced expression of StAR mRNA.
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Cell Line:NCI-H295R human adrenocortical cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly and dose-dependently enhanced the dbcAMP-induced expression of StAR protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:UM-X7.1 hamsters and gold hamsters[1]
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Dosage:0.1% in diet
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Administration:p.o. 4 weeks
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Result:Showed an increase in body weight with no remarkable increase in the biventricular-to-body weight ratio in UM-X7.1 hamsters but not affected the ratio of gold hamsters.
Did not affect the expression of TCCa1G mRNA in either the golden and UM-X7.1 hamster.
Increased left ventricular ejection fraction (LVEF) in UM-X7.1 hamster.
Did not significantly affect blood pressure in either UM X7.1 hamsters or golden hamsters.
Reduced heart rate by approximately 10%.
Significantly lowered the BNP level in UM X7.1 hamsters (from 35.2 pg/ml to 30.5 pg/ml), and the BNP level did not differ significantly in golden hamster group.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 111011-63-3
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性状 Solid
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分子量 631.66
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分子式 C34H38N3O7P
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Color Off-white to yellow
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SMILES
CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1
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別名
NZ-105; (±)-Efonidipine
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Basic Clin Pharmacol Toxicol
A New Method for Antispastic Effect in Coronary Artery Bypass Grafts by Using a L- and T-Type Calcium Channel Blocker Efonidipine. [Abstract]2025 Aug;137(2):e70077. PMID: 40624735
溶剤 & 溶解度
DMSO : 100 mg/mL (158.31 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (3.96 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 (281 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ikeda K, et al. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011;224(4):263-71. [Content Brief]
[2]. Nakano N, et al. Effects of efonidipine, an L- and T-type calcium channel blocker, on the renin-angiotensin-aldosterone system in chronic hemodialysis patients. Int Heart J. 2010 May;51(3):188-92. [Content Brief]
[3]. Suzuki S, et al. Beneficial effects of the dual L- and T-type Ca2+ channel blocker efonidipine on cardiomyopathic hamsters. Circ J. 2007 Dec;71(12):1970-6. [Content Brief]
[4]. Lee TS, et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5831 mL | 7.9157 mL | 15.8313 mL | 39.5783 mL |
| 5 mM | 0.3166 mL | 1.5831 mL | 3.1663 mL | 7.9157 mL | |
| 10 mM | 0.1583 mL | 0.7916 mL | 1.5831 mL | 3.9578 mL | |
| 15 mM | 0.1055 mL | 0.5277 mL | 1.0554 mL | 2.6386 mL | |
| 20 mM | 0.0792 mL | 0.3958 mL | 0.7916 mL | 1.9789 mL | |
| 25 mM | 0.0633 mL | 0.3166 mL | 0.6333 mL | 1.5831 mL | |
| 30 mM | 0.0528 mL | 0.2639 mL | 0.5277 mL | 1.3193 mL | |
| 40 mM | 0.0396 mL | 0.1979 mL | 0.3958 mL | 0.9895 mL | |
| 50 mM | 0.0317 mL | 0.1583 mL | 0.3166 mL | 0.7916 mL | |
| 60 mM | 0.0264 mL | 0.1319 mL | 0.2639 mL | 0.6596 mL | |
| 80 mM | 0.0198 mL | 0.0989 mL | 0.1979 mL | 0.4947 mL | |
| 100 mM | 0.0158 mL | 0.0792 mL | 0.1583 mL | 0.3958 mL |
Efonidipine 関連分類
HY-12502 関連分類
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