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Diltiazem hydrochloride

Name: Diltiazem hydrochloride
Brand: TargetMol
SKU: T0112
Price: 46 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0112Cas No. 33286-22-5

Alias RG 83606 HCl, Diltiazem HCl, CRD-401

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

Diltiazem hydrochloride

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Purity: 99.65%

Catalog No. T0112Alias RG 83606 HCl, Diltiazem HCl, CRD-401Cas No. 33286-22-5

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

Pack Size	Price	USA Warehouse	Global Warehouse
500 mg	$46	-	In Stock
1 g	$53	-	In Stock
5 g	$119	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.65%

Color:White

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Product Introduction

Bioactivity

Description	Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
In vitro	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].
In vivo	Diltiazem exhibits noncompetitive inhibition of calcium-induced contractions in depolarized rabbit aorta and lacks parallel effects between the removal of extracellular calcium ([Ca2+]ex) and its addition. It enhances cardiac microcirculation and function in hyperthyroid rat models, significantly reducing left ventricular fibrosis when combined with losartan (4.7±0.7%; P < 0.001). In spontaneously hypertensive rats, diltiazem lowers blood pressure and increases heart rate in a dose-dependent manner after intravenous administration (0.03--1 mg/kg) and through oral administration (100 mg/kg), demonstrating its therapeutic potential in hypertension management.
Synonyms	RG 83606 HCl, Diltiazem HCl, CRD-401

Chemical Properties

Molecular Weight	450.98
Formula	C₂₂H₂₇ClN₂O₄S
Cas No.	33286-22-5
Smiles	Cl.COc1ccc(cc1)[C@@H]1Sc2ccccc2N(CCN(C)C)C(=O)[C@@H]1OC(C)=O
Relative Density.	1.30 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 100 mg/mL (221.74 mM), Sonication is recommended.

DMSO: 50 mg/mL (110.87 mM), Sonication is recommended.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.2174 mL	11.0870 mL	22.1739 mL	110.8697 mL
5 mM	0.4435 mL	2.2174 mL	4.4348 mL	22.1739 mL
10 mM	0.2217 mL	1.1087 mL	2.2174 mL	11.0870 mL
20 mM	0.1109 mL	0.5543 mL	1.1087 mL	5.5435 mL
50 mM	0.0443 mL	0.2217 mL	0.4435 mL	2.2174 mL
100 mM	0.0222 mL	0.1109 mL	0.2217 mL	1.1087 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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