| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
Azelnidipine (also called UR-12592, CS 905, Calblock and CCRIS 8650), a novel dihydropyridine derivative, is a 3rd generation and long-acting L-type calcium channel blocker, and an antihypertensive drug sold in Japan by Daiichi-Sankyo pharmaceuticals, Inc. Acute administration of azelnidipine prevents a sudden drop of cardiac function after acute stress. Unlike other L-type calcium channel blockers, azelnidipine causes minimal stimulation of the sympathetic nervous system despite its significant depressor effect. Azelnidipine may have a protective role in inflammation in atherosclerosis.
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral azenidipine is rapidly absorbed in a dose-dependent manner. One study showed that after a single oral dose of 4 mg of 14C-labeled azenidipine in humans, approximately 26% of the drug was excreted in the urine and 63% in the feces within one week. A Chinese study investigated the pharmacokinetics of this drug and found its volume of distribution to be 1749 ± 964. Metabolism/Metabolites Like most drugs in its class, azenidipine is primarily metabolized via first-pass metabolism in the liver. Azenidipine is metabolized by hepatic cytochrome P450 (CYP) 3A4, with no active metabolites. It may interact with other drugs or substrates of this enzyme. Azenidipine is lipophilic and has a strong affinity for vascular smooth muscle cell membranes. Biological Half-Life 16–28 hours. |
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| Toxicity/Toxicokinetics |
Protein Binding
Azenidipine binds extensively to human plasma proteins (90%–91%). |
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| References |
Hypertens Res.2003 Mar;26(3):201-8;Int J Pharm.2008 Mar 3;351(1-2):55-60.
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| Additional Infomation |
Azenidipine is an isopropyl ester. Azenidipine is a dihydropyridine calcium channel blocker. It is marketed by Daiichi Sankyo Pharmaceutical Co., Ltd. of Japan. Unlike some other calcium channel blockers, azenidipine has a slow onset of action, provides sustained blood pressure reduction, and only slightly increases heart rate. Its application in the treatment of ischemic stroke is currently under investigation. Indications: For the treatment of hypertension. Mechanism of Action: Azenidipine inhibits transmembrane Ca2+ influx through voltage-dependent channels in the vascular smooth muscle. Ca2+ channels are classified into several types, including L-type, T-type, N-type, P/Q-type, and R-type Ca2+ channels. L-type Ca2+ channels. Under normal circumstances, calcium ions induce smooth muscle contraction, leading to hypertension. When calcium channels are blocked, vascular smooth muscle cannot contract, resulting in relaxation of the vascular smooth muscle wall and a decrease in blood pressure.
Pharmacodynamics Azenidipine is a vasodilator that gradually lowers blood pressure in hypertensive patients. Unlike other drugs in its class, azenidipine does not induce reflex tachycardia due to vasodilation. This is likely due to its gradual blood pressure reduction. Azenidipine also has a sustained antihypertensive effect and, due to its high affinity for vascular tissue and antioxidant activity, has been shown to have a potent anti-atherosclerotic effect. Clinical studies have shown that azenidipine significantly reduces heart rate and proteinuria in hypertensive patients by inhibiting sympathetic nerve activity. Azenidipine has also been shown to have cardioprotective, neuroprotective, and anti-atherosclerotic effects, and has also been found to prevent insulin resistance. |
| Molecular Formula |
C33H34N4O6
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|---|---|
| Molecular Weight |
582.65
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| Exact Mass |
582.247
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| CAS # |
123524-52-7
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| Related CAS # |
Azelnidipine-d7
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| PubChem CID |
65948
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
709.3±60.0 °C at 760 mmHg
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| Melting Point |
120-126ºC
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| Flash Point |
382.8±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
4.21
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
43
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZKFQEACEUNWPMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H34N4O6/c1-20(2)42-32(38)27-21(3)35-31(34)29(28(27)24-15-10-16-25(17-24)37(40)41)33(39)43-26-18-36(19-26)30(22-11-6-4-7-12-22)23-13-8-5-9-14-23/h4-17,20,26,28,30,35H,18-19,34H2,1-3H3
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| Chemical Name |
3-(1-benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
UR-12592; UR-12592; UR-12592; CS 905; CS-905; CS905; CCRIS 8650; CCRIS8650; CCRIS-8650; Azelnidipine; trade name CalBlock.
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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 |
| 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: ≥ 2.5 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 1.7163 mL | 8.5815 mL | 17.1630 mL | |
| 5 mM | 0.3433 mL | 1.7163 mL | 3.4326 mL | |
| 10 mM | 0.1716 mL | 0.8581 mL | 1.7163 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 |
| NCT00294567 | Completed | Drug: Calcium channel blockers (amlodipine, azelnidipine) |
Hypertension Coronary Atherosclerosis |
Juntendo University | December 2005 | Phase 4 |
| NCT01028534 | Completed | Drug: Olmesartan and Azelnidipine | Obstructive Sleep Apnea Hypertension |
Kyoto University, Graduate School of Medicine |
July 2010 | Not Applicable |
| NCT00607035 | Completed | Drug: Olmesartan medoxomil ＋Azelnidipine |
Hypertension | Jichi Medical University | May 2006 | Phase 4 |
| NCT00454662 | Completed | Drug: olmesartan medoxomil / amlodipine or azelnidipine |
Hypertension Cardiovascular Disease |
COLM Study Research Organization | April 2007 | Phase 4 |
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