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

Size Price Stock Quantity
100 mg USD 50 In-stock
500 mg USD 120 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Diltiazem:

Diltiazem Related Antibodies

Top Publications Citing Use of Products

View All Calcium Channel Isoform Specific Products:

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

  • 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

 

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
163 μM
Compound: diltiazem
Antiproliferative activity against human A2780 cells after 3 days by MTT assay
Antiproliferative activity against human A2780 cells after 3 days by MTT assay
[PMID: 19093883]
A2780 ADR IC50
49 μM
Compound: Diltiazem
Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
[PMID: 19250834]
CHO IC50
0.76 μM
Compound: diltiazem
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HEK293 IC50
12.4 μM
Compound: diltiazem
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HEK293 IC50
44 μM
Compound: Diltiazem
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
Ventricular myocyte IC50
0.63 μM
Compound: Diltiazem
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
30 μM
Compound: Diltiazem
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
74 μM
Compound: Diltiazem
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
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: 99.70%

SDS (392 KB)

COA (257 KB) HNMR (234 KB) LCMS (94 KB) OR (214 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Diltiazem
Cat. No.:
HY-B0632
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.