Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Purity: ≥98%
Amlodipine (formerly UK48340; trade name Norvasc among others), a marketed antihypertensive drug, is a long-acting L-type calcium channel blocker/CCB of the dihydropyridine/DHP class. It is an approved medication that has been widely used to treat high blood pressure.
ln Vitro |
In A431 cells, amlodipine (20–40 μM; 48 h) decreases BrdU incorporation to 68.6% and 26.3% at 20 and 30 μM, respectively[3]. Amlodipine (30 μM; pretreatment for 1 h) greatly reduces the increases in [Ca2+]i in A431 cells caused by uridine 5′-triphosphate (UTP)[3]. In cells loaded with Fluo-3, amlodipine (30 μM) suppresses the store-operated Ca2+influx triggered by thapsigargin[3].
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ln Vivo |
In VSMC ATP2B1 KO mice, amlodipine (5 mg/kg/day; sc for 2 weeks) significantly lowers systolic blood pressure (SBP)[4]. ?Amlodipine (10 mg/kg; intraperitoneal; once daily for 20 days) significantly slows 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]. Kishen G. Bulsara, et al. Amlodipine.
[2]. 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. [3]. 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. [4]. 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. |
Molecular Formula |
C20H25CLN2O5
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Molecular Weight |
408.88
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Exact Mass |
408.15
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Elemental Analysis |
C, 58.75; H, 6.16; Cl, 8.67; N, 6.85; O, 19.57
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CAS # |
88150-42-9
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Related CAS # |
Amlodipine maleate;88150-47-4;Amlodipine besylate;111470-99-6;Amlodipine mesylate;246852-12-0;Amlodipine-1,1,2,2-d4 maleate;1185246-15-4;Amlodipine-d4;1185246-14-3
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Appearance |
Solid powder
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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]
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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 |
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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: ≥ 3 mg/mL (7.34 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 30.0 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: 3 mg/mL (7.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 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: ≥ 3 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4457 mL | 12.2285 mL | 24.4571 mL | |
5 mM | 0.4891 mL | 2.4457 mL | 4.8914 mL | |
10 mM | 0.2446 mL | 1.2229 mL | 2.4457 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 |
NCT06193044 | Not yet recruiting | Drug:Amlodipine/Valsartan | Healthy Volunteer | International Bio service | May 7, 2024 | Phase 1 |
NCT01835418 | Unknown | Drug:Amlodipine | Hypertension | Allina Health System | April 2013 | Not Applicable |
NCT04554303 | Unknown | Drug: S-amlodipine 2.5mg Drug: Amlodipine 5mg |
Essential Hypertension | Ahn-Gook Pharmaceuticals Co.,Ltd | October 28, 2020 | |
NCT03294070 | Unknown | Arterial Hypertension | Recurrent Glioma Refractory Glioma |
Centro Universitario de Ciencias de la Salud, Mexico |
September 2017 | Phase 4 |
NCT05667818 | Not yet recruiting | Drug: Amlodipine besylate tablets | Hypertension | Overseas Pharmaceuticals, Ltd. | January 28, 2023 | Phase 1 |
Changes in SBP produced by a single injection of anti-hypertensive drugs. (a) Delta SBP in response to the administration of nicardipine (1 mg kg−1, i.p., n=7 for each group). (b) Delta SBP in response to the administration of candesartan (10 mg kg−1, i.p., n=8 for each group). (c) Delta SBP in response to the administration of prazosin (1 mg kg−1, i.p., n=6 for each group). (d) Delta SBP in response to the administration of amlodipine (5 mg kg−1, i.p., n=8 for each group). (e) Delta SBP in response to the administration of nicardipine every 6 h. The data are means±s.e.m. of each group. *P<0.05 vs. the control group. **P<0.01 vs. the control group. Each arrow indicates the time of drug injection. A horizontal line shows the time after (or before) injection and each injection was at ~15:00. C, control mice; K, VSMC ATP2B1 KO mice. Hypertens Res . 2018 Feb;41(2):80-87. td> |
SBP shifts produced by long-term administration of amlodipine and candesartan measured by the tail-cuff method. (a) SBP and (b) Delta SBP from the baseline in mice administered amlodipine for 2 weeks (5 mg kg−1 per day, s.c., n=9 for each group). (c) SBP and (d) Delta SBP from the baseline in mice administered candesartan for 2 weeks (0.5 mg kg−1 per day, s.c., n=7 for each group). The data are means±s.e.m. of group. *P<0.05 vs. the control group. #P<0.05 vs. own baseline. Hypertens Res . 2018 Feb;41(2):80-87. td> |
SBP shifts produced by amlodipine administration on days 2, 3, 7, and 14 were examined by radio telemetric measurement. (a) Changes in delta SBP of mice treated with amlodipine (5 mg kg−1 per day, s.c., n=6–8). Circadian patterns of SBP of (b) Control and (c) VSMC ATP2B1 KO mice treated with amlodipine for 1 week, measured by the radio telemetric method. Basal SBPs were also measured (n=6–8). 12-h light (8:00 AM to 20:00 PM)/dark (20:00 PM to 8:00 AM) cycle are shown. Values plotted are hourly means. Data are means±s.e.m. of group. *P<0.05 vs. the control group. Hypertens Res . 2018 Feb;41(2):80-87. td> |