Art. -Nr.: HY-B0632

Diltiazem

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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.

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Reinheit: 99.70%
CAS. Nr.: 42399-41-7
Formel: C₂₂H₂₆N₂O₄S
Molecular Weight:414.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Diltiazem Chemical Structure

CAS. Nr.: 42399-41-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

L-type calcium channel

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

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]
LLC-PK1	IC₅₀	77.7 μM Compound: Diltiazem	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]

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.

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 T_1/2 of 61.2 min, CL_el 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:

T_1/2 (61.2 min), CL_el (3.2 mL/min)

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 42399-41-7
Appearance Solid
Molecular Weight 414.52
Formel C₂₂H₂₆N₂O₄S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

All Bio/Physico-chemical Assay

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Journal Impact Factor

Nat Commun

Small molecule in situ resin capture provides a compound first approach to natural product discovery. [Abstract]

2024 Jun 19;15(1):5230. PMID: 38898025
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
J Gen Physiol

Opening of rod photoreceptor CNG channels by photodynamically generated singlet oxygen. [Abstract]

2026 May 4;158(3):e202513819. PMID: 41784565
Vet Sci

Antiviral Activity of Diltiazem HCl Against Pseudorabies Virus Infection In Vitro. [Abstract]

2025 Sep 5;12(9):864. PMID: 41012789
J Cardiovasc Transl Res

Quantification of Cardiomyocyte Contraction In Vitro and Drug Screening by MyocytoBeats. [Abstract]

2023 Aug;16(4):758-767. PMID: 36715820

Diltiazem purchased from MedChemExpress. Usage Cited in: J Cardiovasc Transl Res. 2023 Aug;16(4):758-767. [Abstract]

Representative beating curves of NRVC exposed to Diltiazem (100 nM) or PBS for 24 h (n = 3) and quantitative analysis of the relative beating rate and intensity of NRVC exposed to Diltiazem (100 nM) or PBS for 0 h and 24 h (n = 3).
Pharmacol Res Perspect

Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]

2021 Oct;9(5):e00879. PMID: 34628723
Pharmacol Res Perspect

Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats. [Abstract]

2020 Apr;8(2):e00575. PMID: 32266794
Virology

Porcine deltacoronavirus (PDCoV) modulates calcium influx to favor viral replication. [Abstract]

2020 Jan 2;539:38-48. PMID: 31670218
medRxiv

2025 May 21.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4124 mL

12.0621 mL

24.1243 mL

5 mM

0.4825 mL

2.4124 mL

4.8249 mL

10 mM

0.2412 mL

1.2062 mL

2.4124 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 5 mg/mL (12.06 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (12.06 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yoshinari Niimi, et al. Diltiazem facilitates inactivation of single L-type calcium channels in guinea pig ventricular myocytes. Jpn Heart J. 2003 Nov;44(6):1005-14. [Content Brief]

[2]. S Lin Tang, et l. Structural Basis for Diltiazem Block of a Voltage-Gated Ca2+ Channel. Mol Pharmacol. 2019 Oct; 96(4): 485-492. [Content Brief]

[3]. Anja Mieth , et al. L-type calcium channel inhibitor diltiazem prevents aneurysm formation by blood pressure-independent anti-inflammatory effects. Hypertension. 2013 Dec;62(6):1098-104. [Content Brief]

[4]. S. J. Downing, et al. Diltiazem pharmacokinetics in the rat and relationship between its serum concentration and uterine and cardiovascular effects. Br J Pharmacol. 1987 Aug; 91(4): 735-745. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Diltiazem

10 Cited Publications

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Diltiazem

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Publications Citing Use of MedChemExpress (MCE) Diltiazem

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Diltiazem

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Rare Diseases Drug Library

Calcium Channel Blocker Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Off-patent Drug Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Diltiazem

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Diltiazem Related Classifications

HY-B0632 Related Classifications