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Purity: ≥98%
Diltiazem HCl (Tiazac, RG-83606 HCl) is a benzothiazepine derivative and a calcium-channel blocker (CCB) with vasodilating activity. It is an approved medication that has been used to treat hypertension, angina, and arrhythmia. Diltiazem is chemically classified as a nondihydropyridines (non-DHP) CCB. It acts by relaxing the smooth muscles in the walls of arteries, which opens (dilates) the arteries, allows blood to flow more easily, and lowers blood pressure.
| ln Vitro |
The α1 subunit of L-type Ca2+ channels interacts with transmembrane segments IIIS6 and IVS6 in the benzothiazepine Ca2+ antagonist diltiazem hydrochloride[1]. In addition to stimulating Ca2+ influx that is triggered by alpha adrenoceptor activation and high-K+ depolarization, diltiazem also inhibits contractions in a dose-dependent manner. When it comes to preventing contractions brought on by high K+ and low norepinephrine (NE) concentrations, diltiazem is about equally effective[2]. Additionally, the Na-dependent Ca-efflux from cardiac mitochondria is inhibited by diltiazem. Diltiazem's cis- and trans-optical (+)-optical isomers both block Na-Ca exchange activity with a similar degree of potency (IC50 of 10–20 μM)[3].
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| ln Vivo |
The noncompetitive suppression of Ca2+-induced contractions in the depolarized rabbit aorta is achieved by diltiazem. Moreover, the effects on smooth muscle caused by adding diltiazem and removing [Ca2+]ex are not parallel[2]. Diltiazem enhances heart microcirculation and function in a rat hyperthyroidism experimental paradigm. Losartan diltiazem therapy significantly lowers the proportion of fibrosis regions in the left ventricle (4.7±0.7%; P < 0.001) in hyperthyroid rats [4]. Diltiazem is administered intravenously (0.03–-1 mg/kg) to conscious spontaneously hypertensive rats (SHR), and it dose-dependently lowers blood pressure and raises heart rate. SHR blood pressure is also lowered by oral diltiazem treatment (100 mg/kg)[5].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Based on limited data, amounts of diltiazem ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| Additional Infomation |
Diltiazem Hydrochloride can cause developmental toxicity according to state or federal government labeling requirements.
Diltiazem hydrochloride is a hydrochloride salt resulting from the reaction of equimolar amounts of diltiazem and hydrogen chloride. A calcium-channel blocker and vasodilator, it is used in the management of angina pectoris and hypertension. It has a role as an antihypertensive agent, a vasodilator agent and a calcium channel blocker. It contains a diltiazem(1+). It is an enantiomer of an ent-diltiazem hydrochloride. Diltiazem Hydrochloride is a benzothiazepine calcium channel blocking agent. Diltiazem hydrochloride inhibits the transmembrane influx of extracellular calcium ions into select myocardial and vascular smooth muscle cells, causing dilatation of coronary and systemic arteries and decreasing myocardial contractility. Because of its vasodilatory activity, this agent has been shown to improve the microcirculation in some tumors, thereby potentially improving the delivery of antineoplastic agents to tumor cells. (NCI04) A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. See also: Diltiazem (has active moiety). Drug Indication Treatment of chronic anal fissure |
| Molecular Formula |
C22H26N2O4S.HCL
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| Molecular Weight |
450.98
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| Exact Mass |
450.138
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| CAS # |
33286-22-5
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| Related CAS # |
Diltiazem-d3 hydrochloride;1217623-80-7;Diltiazem;42399-41-7;Diltiazem-(acetoxy-d3) (hydrochloride);1217860-13-3
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| PubChem CID |
62920
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| Appearance |
White to off-white solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
594.4ºC at 760mmHg
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| Melting Point |
212-214 °C
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| Flash Point |
313.3ºC
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| Index of Refraction |
118 ° (C=1, H2O)
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| LogP |
4.235
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
565
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=O)O[C@@H]1[C@@H](SC2=CC=CC=C2N(C1=O)CCN(C)C)C3=CC=C(C=C3)OC.Cl
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| InChi Key |
HDRXZJPWHTXQRI-BHDTVMLSSA-N
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| InChi Code |
InChI=1S/C22H26N2O4S.ClH/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3;/h5-12,20-21H,13-14H2,1-4H3;1H/t20-,21+;/m1./s1
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| Chemical Name |
[(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (221.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2174 mL | 11.0870 mL | 22.1739 mL | |
| 5 mM | 0.4435 mL | 2.2174 mL | 4.4348 mL | |
| 10 mM | 0.2217 mL | 1.1087 mL | 2.2174 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02080780 | Completed Has Results | Drug: Clarithromycin XL Drug: 2% Diltiazem |
CLARITHROMYCIN/DILTIAZEM [VA Drug Interaction] |
Ventrus Biosciences, Inc | September 2013 | Phase 1 |
| NCT04777045 | Active, not recruiting | Drug: Diltiazem Hydrochloride Drug: Placebo |
Microvascular Angina Coronary Vasospasm |
Radboud University Medical Center | October 25, 2019 | Phase 3 |
| NCT03472495 | Completed Has Results | Drug: Diltiazem Oral Product Drug: Diltiazem Injectable Product |
Atrial Fibrillation and Flutter | Virginia Commonwealth University | June 1, 2018 | Phase 4 |
| NCT05563168 | Withdrawn | Drug: DILTIAZEM TEVA 60 mg or placebo |
COVID-19 | Hospices Civils de Lyon | April 2023 | Phase 2 |
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