Diltiazem hydrochloride
Based on 10 publication(s) in Google Scholar
Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).
For research use only. We do not sell to patients.
- Purity: 99.47%
- CAS No.: 33286-22-5
- Formula: C22H27ClN2O4S
- Molecular Weight:450.98
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Diltiazem hydrochloride
More- Nat Commun. 2024 Jun 19;15(1):5230. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Gen Physiol. 2026 May 4;158(3):e202513819. [Abstract]
- J Cardiovasc Transl Res. 2023 Aug;16(4):758-767. [Abstract]
- Virology. 2020 Jan 2;539:38-48. [Abstract]
- Vet Sci. 2025 Sep 5;12(9):864. [Abstract]
- Pharmacol Res Perspect. 2021 Oct;9(5):e00879. [Abstract]
- Pharmacol Res Perspect. 2020 Apr;8(2):e00575. [Abstract]
- medRxiv. 2025 May 21.
All Calcium Channel Isoforms
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Biological Activity
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L-type calcium channel |
Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels[1].
Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K+ and a low concentration of norepinephrine (NE)[2].
Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC50 of 10-20 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 33286-22-5
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Appearance Solid
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Molecular Weight 450.98
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Formula C22H27ClN2O4S
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Color White to off-white
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SMILES
CN(C)CCN1C2=CC=CC=C2S[C@@H](C3=CC=C(OC)C=C3)[C@@H](OC(C)=O)C1=O.Cl
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Synonyms
CRD-401
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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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
2026 May 4;158(3):e202513819. PMID: 41784565 -
J Cardiovasc Transl Res
2023 Aug;16(4):758-767. PMID: 36715820 -
Virology
2020 Jan 2;539:38-48. PMID: 31670218 -
Vet Sci
2025 Sep 5;12(9):864. PMID: 41012789 -
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 -
Solvent & Solubility
H2O : 33.33 mg/mL (73.91 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (221.74 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12. [Content Brief]
[2]. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63. [Content Brief]
[3]. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40. [Content Brief]
[4]. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40. [Content Brief]
[5]. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (author's transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106. [Content Brief]
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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.2174 mL | 11.0870 mL | 22.1739 mL | 55.4348 mL |
| 5 mM | 0.4435 mL | 2.2174 mL | 4.4348 mL | 11.0870 mL | |
| 10 mM | 0.2217 mL | 1.1087 mL | 2.2174 mL | 5.5435 mL | |
| 15 mM | 0.1478 mL | 0.7391 mL | 1.4783 mL | 3.6957 mL | |
| 20 mM | 0.1109 mL | 0.5543 mL | 1.1087 mL | 2.7717 mL | |
| 25 mM | 0.0887 mL | 0.4435 mL | 0.8870 mL | 2.2174 mL | |
| 30 mM | 0.0739 mL | 0.3696 mL | 0.7391 mL | 1.8478 mL | |
| 40 mM | 0.0554 mL | 0.2772 mL | 0.5543 mL | 1.3859 mL | |
| 50 mM | 0.0443 mL | 0.2217 mL | 0.4435 mL | 1.1087 mL | |
| 60 mM | 0.0370 mL | 0.1848 mL | 0.3696 mL | 0.9239 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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