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2g |
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5g |
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10g |
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Purity: ≥98%
Amlodipine (formerly UK-48340; Norvasc; used as as besylate, mesylate or maleate salts) is a selective and long-acting CCB-calcium channel blocker that belongs to the dihydropyridine (DHP) class. It is a anti-hypertensive medication used to lower blood pressure and prevent chest pain. Amlodipine causes a dose-dependent increase in nitrite production. Amlodipine also increases nitrite production in large coronary arteries and in aorta. Amlodipine is attributed to distinct membrane physico-chemical interactions.
ln Vitro |
In A431 cells, amlodipine besylate (20–40 μM; 48 h) decreases BrdU incorporation to 68.6% and 26.3% at 20 and 30 μM, respectively[3]. In A431 cells, uridine 5′-triphosphate (UTP)-induced elevations in [Ca2+]i are greatly attenuated by amlodipine besylate (30 μM; pretreatment for 1 hour)[3]. In cells loaded with Fluo-3, amlodipine besylate (30 μM) suppresses the store-operated Ca2+influx triggered by thapsigargin[3].
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ln Vivo |
In VSMC ATP2B1 KO mice, amlodipine besylate (5 mg/kg/day; sc for 2 weeks) significantly lowers systolic blood pressure (SBP)[4]. The treatment of amlodipine besylate (10 mg/kg; intraperitoneal; once daily for 20 days) significantly inhibits the formation of tumors and increases the longevity of A431 tumor-bearing mice[3].
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Animal Protocol |
Animal/Disease Models: ATP2B1loxP/loxP mice[4]
Doses: 5 mg/kg/day Route of Administration: subcutaneously (sc) implanted osmotic pump for 2 weeks Experimental Results: Dramatically diminished the blood pressure. |
References |
[1]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.
[2]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87. [3]. Kishen G. Bulsara, et al. Amlodipine. [4]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586. |
Molecular Formula |
C20H25CLN2O5.C6H6O3S
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Molecular Weight |
567.05
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CAS # |
111470-99-6
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Related CAS # |
Amlodipine;88150-42-9;Amlodipine maleate;88150-47-4;Amlodipine-d4 besylate;Amlodipine mesylate;246852-12-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1C1([H])C(C(=O)OC([H])([H])[H])=C(C([H])([H])[H])N([H])C(C([H])([H])OC([H])([H])C([H])([H])N([H])[H])=C1C(=O)OC([H])([H])C([H])([H])[H].S(C1C([H])=C([H])C([H])=C([H])C=1[H])(=O)(=O)O[H]
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InChi Key |
ZPBWCRDSRKPIDG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H25ClN2O5.C6H6O3S/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21;7-10(8,9)6-4-2-1-3-5-6/h5-8,17,23H,4,9-11,22H2,1-3H3;1-5H,(H,7,8,9)
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Chemical Name |
3,5-Pyridinedicarboxylic acid, 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester, (+-)-, monobenzenesulfonate
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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: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.41 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (3.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7635 mL | 8.8176 mL | 17.6351 mL | |
5 mM | 0.3527 mL | 1.7635 mL | 3.5270 mL | |
10 mM | 0.1764 mL | 0.8818 mL | 1.7635 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 |
NCT02353806 | Completed Has Results | Drug: Amlodipine besylate | Chronic Hypertension in Pregnancy | University of Texas Southwestern Medical Center |
January 2015 | Phase 4 |
NCT05667818 | Not yet recruiting | Drug: Amlodipine besylate tablets (trade name: Norfloxacin ®) | Hypertension | Overseas Pharmaceuticals, Ltd. | January 28, 2023 | Phase 1 |
NCT01155908 | Completed | Drug: Amlodipine Besylate / Benazepril Hydrochloride |
Healthy | Dr. Reddy's Laboratories Limited | April 2005 | Phase 1 |
NCT02940548 | Terminated | Drug: Nifedipine GITS Drug: Amlodipine besylate |
Hypertension | Jing Liu | December 2016 | Phase 4 |