Cat. No.: HY-B0632

Diltiazem

Name: Diltiazem
Brand: MedChemExpress
SKU: HY-B0632
Price: 50.00 USD
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11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Diltiazem is a calcium antagonist and an L-type calcium channel inhibitor. Diltiazem inhibits Ca²⁺ mobilization/influx, norepinephrine-induced contraction, and depolarization. Diltiazem produces coronary vasodilation and renal vasodilation; it inhibits sodium reabsorption in the distal nephron and increases urine flow, sodium and potassium excretion, Inulin (HY-N7075) and PAH clearance, and free water clearance. Diltiazem is used in research on cardiovascular diseases, kidney diseases, and inflammation.

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Pureté : 99.70%
CAS No.: 42399-41-7
Formule: C₂₂H₂₆N₂O₄S
Masse moléculaire:414.52

Stockage:

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

Diltiazem Chemical Structure

CAS No.: 42399-41-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[4]

L-type calcium channel

Voir tous les produits spécifiques à Isoform 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]
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

Local Vascular Regulation

Diltiazem (CRD-401) produces stronger inhibition of nerve-evoked contractions than of direct muscle-evoked contractions in rabbit mesenteric and pulmonary arteries, reducing the pulmonary nerve response to 10% of control^[3].
Diltiazem reduces depolarization-induced contraction in voltage-clamped rabbit main pulmonary artery^[3].
Diltiazem reduces norepinephrine-induced contraction of rabbit main pulmonary artery and inhibits norepinephrine-induced depolarization^[3].
Diltiazem increases the K⁺-induced mechanical threshold in rabbit main pulmonary arteries and reduces K⁺-induced contraction^[3].

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

In Vivo

Local Vascular RegulationOxidative StressRenal RegulationCardiovascular Regulation

Local Vascular Regulation

Diltiazem (CRD-401) (3 µg/kg; intra-arterial administration; single injection) produces a stronger and longer-lasting coronary vasodilatory effect than its l-isomer in anesthetized dogs^[1].

Oxidative Stress

Diltiazem inhibits interleukin-6-mediated AP-1 promoter activity in macrophages, exerts a blood pressure-independent anti-inflammatory effect, and inhibits the formation of aortic aneurysms in angiotensin-II-infused ApoE^-/- mouse models^[4].

Renal Regulation

Diltiazem (1-30 μg/kg/min; continuous intrarenal arterial infusion) increases urinary flow rate, sodium excretion, and renal blood flow under saline and water diuresis conditions, and increases glomerular filtration rate under saline loading, but does not increase it under water diuresis conditions^[2].
Diltiazem (10 μg/kg/min; continuous intrarenal arterial infusion) increases sodium excretion even when renal blood flow is maintained constant by aortic clamping; and it reduces sodium reabsorption in the distal nephron^[2].

Renal Regulation

Local Vascular Regulation

Cardiovascular Regulation

Diltiazem (CRD-401) (1-100 μg/kg; intrarenal arterial bolus injection; intravenous bolus injection; continuous intrarenal arterial infusion) increases renal blood flow through direct renal vasodilation^[2].

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

Related Protocols :

Essai clinique

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

Chemical Information

CAS No. 42399-41-7
Appearance Solid
Masse moléculaire 414.52
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (11)

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
Immunobiology

2026 Sep;231(5):153237. PMID: 42664531
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.

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 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)
Instruction de manipulation (2659 KB)

Références

[1]. Nagao T, et al. Studies on a New 1,5-Benzothiazepine Derivative (CRD-401). IV. Coronary Vasodilating Effect and Structure-Activity Relationship. Chemical and Pharmaceutical Bulletin, 1973, 21(1): 92-97.

[2]. Yamaguchi I, et al. Studies on a New 1,5-Benzothiazepine Derivative (CRD-401): VI. Effects on Renal Blood Flow and Renal Function. Japanese Journal of Pharmacology, 1974, 24(4): 511-522.

[3]. Ito Y, et al. The effects of diltiazem (CRD-401) on the membrane and mechanical properties of vascular smooth muscles of the rabbit. British journal of pharmacology. 1978 Dec;64(4):503-10.

[4]. Mieth A, 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]

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

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Keywords

Diltiazem

11 Cited Publications

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Diltiazem

Publications Citing Use of MedChemExpress (MCE) Diltiazem

Voir tous les produits spécifiques à Isoform Calcium Channel