2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Diltiazem

Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

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

Diltiazem Chemical Structure

Diltiazem Chemical Structure

CAS No. : 42399-41-7

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Based on 4 publication(s) in Google Scholar

Other Forms of Diltiazem:

Diltiazem Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].

IC50 & Target

L-type calcium channel

 

In Vitro

Diltiazem (200 µM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses[1].
Diltiazem reduces Ca2+ influx by accelerating inactivation during action potentials, and that the use-dependent blockade is due to increases in the number of channels in a sustained closed state[1].

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

Diltiazem Related Antibodies
In Vivo

Diltiazem (100 mg/kg; p.o.; for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner[3].
Diltiazem limits aortic aneurysm formation in mice by a blood pressure-independent anti-inflammatory effect on monocytic cells[3].
Diltiazem (2 mg/kg; i.v.) exhibits T1/2 of 61.2 min, CLel of 3.2 mL/min in rats[4].

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

Animal Model: Male ApoE−/− mice, angiotensin II induced aneurysms[3]
Dosage: 100 mg/kg
Administration: Oral administration, in drinking water, for 4 weeks
Result: Srongly reduced the vascular remodeling but also lowered the blood pressure.
Animal Model: Rat (200-250 g)[4]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: Intravenous injection
Result: T1/2 (61.2 min), CLel (3.2 mL/min)
Clinical Trial
Molecular Weight

414.52

Formula

C22H26N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCN1C2=CC=CC=C2S[C@@H](C3=CC=C(OC)C=C3)[C@@H](OC(C)=O)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (120.62 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 2.4124 mL 12.0621 mL 24.1243 mL
5 mM 0.4825 mL 2.4124 mL 4.8249 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
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.03 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 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).
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: 99.49%

COA (256 KB) HNMR (272 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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. 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 2.4124 mL 12.0621 mL 24.1243 mL 60.3107 mL
5 mM 0.4825 mL 2.4124 mL 4.8249 mL 12.0621 mL
10 mM 0.2412 mL 1.2062 mL 2.4124 mL 6.0311 mL
15 mM 0.1608 mL 0.8041 mL 1.6083 mL 4.0207 mL
20 mM 0.1206 mL 0.6031 mL 1.2062 mL 3.0155 mL
25 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4124 mL
30 mM 0.0804 mL 0.4021 mL 0.8041 mL 2.0104 mL
40 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5078 mL
50 mM 0.0482 mL 0.2412 mL 0.4825 mL 1.2062 mL
60 mM 0.0402 mL 0.2010 mL 0.4021 mL 1.0052 mL
80 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7539 mL
100 mM 0.0241 mL 0.1206 mL 0.2412 mL 0.6031 mL
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Diltiazem 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:

Diltiazem42399-41-7Calcium ChannelCa2+ channelsCa channelsantihypertensiveantiarrhythmiccardiacarrhythmiahypertensionanginapectorisInhibitorinhibitorinhibit

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