2. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection
  3. Calcium Channel SARS-CoV
  4. Efonidipine

Efonidipine  (Synonyms: NZ-105; (±)-Efonidipine)

製品番号: HY-12502 純度: 99.88%
COA 取扱説明書 Technical Support

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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Efonidipine

Efonidipine 構造式

CAS 番号 : 111011-63-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 63 在庫あり
Solution
10 mM * 1 mL in DMSO USD 63 在庫あり
Solid
5 mg $45 在庫あり
10 mg $72 在庫あり
25 mg $137 在庫あり
50 mg $220 在庫あり
100 mg $353 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of Efonidipine:

Efonidipine 関連抗体

Top Publications Citing Use of Products

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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  • 参考文献

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製品説明

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[1][2][3][4][5].

IC50 & Target

L-type calcium channel

1.8 nM (IC50)

T-type calcium channel

350 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
LLC-PK1 IC50
13 μM
Compound: Efonidipine
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
[PMID: 12128170]
LLC-PK1 IC50
17.3 μM
Compound: Efonidipine
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
[PMID: 11145223]
LLC-PK1 IC50
20.6 μM
Compound: Efonidipine
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
[PMID: 11145223]
体外実験

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.

Efonidipine 関連抗体

RT-PCR[1]

Cell Line: NCI-H295R human adrenocortical cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Dose-dependently and significantly enhanced the dbcAMP-induced expression of StAR mRNA.
Enhanced the angiotensin II-induced expression of StAR mRNA.

Western Blot Analysis[1]

Cell Line: NCI-H295R human adrenocortical cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly and dose-dependently enhanced the dbcAMP-induced expression of StAR protein.
体内実験

Efonidipine (0.1% in diet, p.o., 4 weeks) inhibits T type calcium channels and improves cardiac function during the progression of heart failure in UM-X7.1 hamsters and gold hamsters[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: UM-X7.1 hamsters and gold hamsters[1]
Dosage: 0.1% in diet
Administration: p.o. 4 weeks
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.
臨床実験
分子量

631.66

分子式

C34H38N3O7P
CAS 番号
Appearance

Solid

Color

Off-white to yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5831 mL 7.9157 mL 15.8313 mL
5 mM 0.3166 mL 1.5831 mL 3.1663 mL
10 mM 0.1583 mL 0.7916 mL 1.5831 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (3.96 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

純度: 99.88%

COA (251 KB) HNMR (234 KB) LCMS (92 KB)

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, 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
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Efonidipine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Efonidipine111011-63-3NZ-105(±)-EfonidipineNZ105NZ 105Calcium ChannelSARS-CoVCa2+ channelsCa channelsSARS coronavirusorally activeStARDHEA-Shypertensionheart failureand disorders involving dysregulated steroid hormone synthesisInhibitorinhibitorinhibit

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