1. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis
  2. Calcium Channel Apoptosis
  3. Benidipine hydrochloride

Benidipine hydrochloride  (Synonyms: KW-3049)

Cat. No.: HY-B1448 Purity: 99.80%
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Benidipine hydrochloride is an orally active calcium channel antagonist. Benidipine hydrochloride can inhibit cell proliferation and apoptosis. Benidipine hydrochloride has antioxidant activity and can increase nitric oxide synthase activity and improve coronary circulation in hypertensive rats.

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Benidipine hydrochloride Chemical Structure

Benidipine hydrochloride Chemical Structure

CAS No. : 91599-74-5

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10 mM * 1 mL in DMSO
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Description

Benidipine hydrochloride is an orally active calcium channel antagonist. Benidipine hydrochloride can inhibit cell proliferation and apoptosis. Benidipine hydrochloride has antioxidant activity and can increase nitric oxide synthase activity and improve coronary circulation in hypertensive rats[1][2][3][4][5][6].

In Vitro

Benidipine hydrochloride (0.01-1 μM, 7 days) promotes mouse endothelial cell differentiation by enhancing phosphorylated Akt[5].
Benidipine hydrochloride (0.1-10 μM) inhibits the proliferation of mesangial cells, at both the G0/G1 and G1/S phases[6].

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

Western Blot Analysis[5]

Cell Line: Murine PBMCs
Concentration: 1 μM
Incubation Time: 7 days
Result: Increased the expression of phosphorylated Akt on serine-473.

Cell Proliferation Assay[6]

Cell Line: Mesangial cells
Concentration: 0.1-10 μM
Incubation Time: 48 h
Result: Inhibited the progression of the cell cycle in a dose-dependent manner.
In Vivo

Benidipine hydrochloride (3-10 µg/kg, i.v.) shows a significant anti-apoptotic effect in rabbits, independent of hemodynamics [2].
Benidipine hydrochloride (5 mg/kg, i.v., every day for 6 weeks) increases the activity of endothelial cell-type nitric oxide synthase (eNOS) and improves coronary circulation in hypertensive rats[3].
Benidipine hydrochloride (1-10 mg/kg, p.o., once daily for 1 week) has significant cardioprotective effects against ischemia-reperfusion injury[4].

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

Animal Model: MI/R rabbits model[2]
Dosage: 3-10 μg/kg
Administration: i.v.
Result: Caused a significant decrease in HR ( heart rate), MABP (mean arterial blood pressure), and PRI (pressure-rate index) at 10 µg/kg.
Decreased apoptotic positive cells to 7.4% at 3 µg/kg.
Animal Model: Renovascular hypertensive rats (RHR) model[3]
Dosage: 5 mg/kg
Administration: i.v.
Result: Decreased the blood pressure and coronary vascular resistance index.
Increased nitrite production and eNOS mRNA expression and the coronary flow at rest, the capillary density.
Animal Model: Rat heart model[4]
Dosage: 1-10 mg/kg
Administration: p.o.
Result: Increased the post-ischemic recovery of LVDP and LV dP/dt max (LVDP: 87.5±10.1 vs 64.6±11.9%; LV dP/dt max: 97.8±10.4 vs 70.2±15.7%) at 3 mg/kg.
Clinical Trial
Molecular Weight

542.02

Formula

C28H32ClN3O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C)NC(C)=C(C(O[C@H]2CN(CC3=CC=CC=C3)CCC2)=O)[C@@H]1C4=CC=CC([N+]([O-])=O)=C4)OC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (61.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8450 mL 9.2248 mL 18.4495 mL
5 mM 0.3690 mL 1.8450 mL 3.6899 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 (sealed storage, away from moisture). 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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: ≥ 2.08 mg/mL (3.84 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.84 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.
Purity & Documentation

Purity: 99.80%

References

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 (sealed storage, away from moisture). 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 1.8450 mL 9.2248 mL 18.4495 mL 46.1238 mL
5 mM 0.3690 mL 1.8450 mL 3.6899 mL 9.2248 mL
10 mM 0.1845 mL 0.9225 mL 1.8450 mL 4.6124 mL
15 mM 0.1230 mL 0.6150 mL 1.2300 mL 3.0749 mL
20 mM 0.0922 mL 0.4612 mL 0.9225 mL 2.3062 mL
25 mM 0.0738 mL 0.3690 mL 0.7380 mL 1.8450 mL
30 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5375 mL
40 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1531 mL
50 mM 0.0369 mL 0.1845 mL 0.3690 mL 0.9225 mL
60 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL
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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.

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Benidipine hydrochloride
Cat. No.:
HY-B1448
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