| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
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Diltiazem ((Tiazac; CRD-401; Dilticard; RG83606) is a nondihydropyridines (non-DHP) calcium channel blocker 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 |
Diltiazem (200 µM) causes a use-dependent blockage in a modest number of pulses [1]. Diltiazem lowers Ca2+ inflow by speeding up inactivation during action potentials, and the use-dependent blockage is caused by an increase in the number of channels that remain closed for an extended period of time.
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| ln Vivo |
Aortic aneurysm formation is prevented by diltiazem (100 mg/kg; po; for 4 weeks) in a way that is independent of blood pressure[3]. Diltiazem inhibits the growth of aortic aneurysms in mice via having an anti-inflammatory action on monocytic cells that is independent of blood pressure[3]. Rats given Diltiazem (2 mg/kg; IV) show T1/2 of 61.2 min and CLel of 3.2 mL/min[4].
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| Animal Protocol |
Animal/Disease Models: Male ApoE−/− mice, angiotensin II induced aneurysms[3]
Doses: 100 mg/kg Route of Administration: Oral administration, in drinking water, for 4 weeks Experimental Results: Srongly decreased the vascular remodeling but also lowered the blood pressure. Animal/Disease Models: Rat (200-250 g)[4] Doses: 2 mg/kg ( pharmacokinetic/PK Analysis) Route of Administration: intravenous (iv) injection Experimental Results: T1/2 (61.2 min), CLel (3.2 mL/min) |
| References |
[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.
[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. [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. [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. |
| Molecular Formula |
C22H26N2O4S
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|---|---|
| Molecular Weight |
414.52
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| Exact Mass |
414.1613
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| CAS # |
42399-41-7
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| Related CAS # |
Diltiazem hydrochloride;33286-22-5;Diltiazem malate;144604-00-2;Diltiazem-d6;1242184-41-3
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| SMILES |
O=C1[C@H](OC(C)=O)[C@H](C2=CC=C(OC)C=C2)SC3=CC=CC=C3N1CCN(C)C
|
| InChi Key |
HSUGRBWQSSZJOP-RTWAWAEBSA-N
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| InChi Code |
InChI=1S/C22H26N2O4S/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/t20-,21+/m1/s1
|
| Chemical Name |
(2S,3S)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate
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| Synonyms |
CRD 401 DiltiazemCRD-401 DilticardCRD401 Dilzen
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~100 mg/mL (~241.24 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*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.
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