2. Membrane Transporter/Ion Channel Neuronal Signaling NF-κB
  3. Calcium Channel NF-κB
  4. Manidipine dihydrochloride

Manidipine dihydrochloride  (Synonyms: CV-4093)

Cat. No.: HY-17403 Purity: 99.91%
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Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.

For research use only. We do not sell to patients.

Manidipine dihydrochloride Chemical Structure

Manidipine dihydrochloride Chemical Structure

CAS No. : 89226-75-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Manidipine dihydrochloride:

Manidipine dihydrochloride Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection[1][2][3][4][5][6].

IC50 & Target

T-type calcium channel

 

In Vitro

Manidipine dihydrochloride (1 μM, 42 h) suppresses IL-6 secretion in lipoproteins-induced HUVEC[3].
Manidipine dihydrochloride (1 μM, 16 h) suppresses IL-6 secretion in 10 ng/mL IL-1, 10 ng/mL IFN-γ, and 25 ng/mL TNFα treated THP-I [3].
Manidipine dihydrochloride (20 mg/mL, 48/20 h) inhibits propagation/genome replication of SFTSV (a negative-strand RNA virus) in SW13 cells[4].
Manidipine dihydrochloride (20 mg/mL, 48 h) interferes SFTSV N-induced inclusion body formation in Huh-7 cells[4].

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

Manidipine dihydrochloride Related Antibodies
In Vivo

Manidipine dihydrochloride (10 mg/kg, i.p., b.i.d. at day 4, day 5) prolongs survival in SFTSV-infected mice[4].
Manidipine dihydrochloride (25 mg/kg, i.p., b.i.d. for 2 d, then daily for 19 d) protects mice from JEV infection[5].
Manidipine dihydrochloride (3 mg/kg, i.g., once per day, 7 d) prevents isoproterenol-induced left ventricular hypertrophy in rats[7].

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

Animal Model: IFNAR-/- mice[4]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p. ), b.i.d. at day 4, day 5
Result: Exhibited a modest, but statistically significant increase in the survival rate of lethal animal model with SFTSV infection, significantly reduced viral titers in the spleen and kidney.
Animal Model: Adult female BALB/c mice (age, 4 weeks) [5]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection (i.p. ), b.i.d. for 2 days, then daily for 19 days
Result: Reduced the mortality rate from 73% to 20%, significantly reduced the viral load in infected mice while remarkably alleviated brain damage phenomena. Had little effect on peripheral JEV infection, which indicated that manidipine protected the mice against JEV-induced lethality by decreasing the viral load in the brain.
Animal Model: 8-week-old male Wistar rats[7]
Dosage: 3 mg/kg
Administration: Intragastric gavage (i.g.), once per day for 7 d
Result: Prevented isoproterenol-induced left ventricular hypertrophy (2.26±0.02 g/kg; p<0.01) as isoproterenol increased left ventricular weight (2.40±0.04 g/kg; p<0.01). Inhibited expression of mRNA of ANP (0.9-fold of the control value; p<0.01), collagen types I (1.1-fold; p<0.01) and type III (1.6-fold; p<0.01), and fibronectin (1.1-fold; p<0.01).
Clinical Trial
Molecular Weight

683.62

Formula

C35H40Cl2N4O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OCCN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3.[H]Cl.[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 : 50 mg/mL (73.14 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 1.4628 mL 7.3140 mL 14.6280 mL
5 mM 0.2926 mL 1.4628 mL 2.9256 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (3.66 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 (3.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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).

*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
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 1.4628 mL 7.3140 mL 14.6280 mL 36.5700 mL
5 mM 0.2926 mL 1.4628 mL 2.9256 mL 7.3140 mL
10 mM 0.1463 mL 0.7314 mL 1.4628 mL 3.6570 mL
15 mM 0.0975 mL 0.4876 mL 0.9752 mL 2.4380 mL
20 mM 0.0731 mL 0.3657 mL 0.7314 mL 1.8285 mL
25 mM 0.0585 mL 0.2926 mL 0.5851 mL 1.4628 mL
30 mM 0.0488 mL 0.2438 mL 0.4876 mL 1.2190 mL
40 mM 0.0366 mL 0.1829 mL 0.3657 mL 0.9143 mL
50 mM 0.0293 mL 0.1463 mL 0.2926 mL 0.7314 mL
60 mM 0.0244 mL 0.1219 mL 0.2438 mL 0.6095 mL
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Manidipine dihydrochloride Related Classifications

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:

Manidipine89226-75-5CV-4093CV4093CV 4093Calcium ChannelNF-κBCa2+ channelsCa channelsNuclear factor-κBNuclear factor-kappaBLipophilicvasoselectivecalcium channel antagonistantihypertensiveanti-inflammatoryflavivirusnegative-strand RNA virusescardiovascularmetabolic diseaseIFNAR2/2 miceBALB/c miceInhibitorinhibitorinhibit

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