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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. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited information indicates that milk levels of amlodipine are usually low and plasma levels in breastfed infants are undetectable. Maternal use of amlodipine during breastfeeding has not caused any adverse effects in breastfed infants. If the mother requires amlodipine, it is not a reason to discontinue breastfeeding. ◉ Effects in Breastfed Infants A woman took amlodipine for hypertension 5 mg daily beginning 2 weeks postpartum. Her exclusively breastfed infant was examined regularly and at 3 months of age was healthy and had normal physical and neurological development. One woman received amlodipine 2.5 mg orally twice daily during pregnancy for hypertension associated with glomerulonephritis. The dose was increased to 5 mg twice daily on day 2 postpartum. Her exclusively breastfed infant's growth was normal throughout the first year of life and no adverse effects were noted. A preterm infant of 32 weeks gestation was breastfed exclusively from day 7 to day 20 postpartum. The infant's mother was taking amlodipine and labetalol in unspecified dosages for hypertension. The infant had apnea episodes unrelated to amlodipine. Growth at 2 months of age was slightly low. Thirty-one women with pregnancy-induced hypertension postpartum received amlodipine 5 mg daily by mouth, with the dosage increased as needed to maintain blood pressure of 140/90 mm Hg or less. Their breastfed (extent not stated) infants exhibited no observed adverse cardiovascular effects within 3 weeks postpartum, although exact measurement methods were not stated. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Amlodipine benzenesulfonate is the benzenesulfonate salt of amlodipine. It has a role as a vasodilator agent, a calcium channel blocker and an antihypertensive agent. It contains an amlodipine.
Amlodipine Besylate is the besylate salt of amlodipine, a synthetic dihydropyridine with antihypertensive and antianginal effects. Amlodipine inhibits the influx of extracellular calcium ions into myocardial and peripheral vascular smooth muscle cells, thereby preventing vascular and myocardial contraction. This results in a dilatation of the main coronary and systemic arteries, decreased myocardial contractility, increased blood flow and oxygen delivery to the myocardial tissue, and decreased total peripheral resistance. This agent may also modulate multi-drug resistance (MDR) activity through inhibition of the p-glycoprotein efflux pump. A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION. See also: Amlodipine (has active moiety); Amlodipine besylate; benazepril hydrochloride (component of); Amlodipine besylate; telmisartan (component of) ... View More ... Drug Indication Treatment of systemic arterial hypertension in cats. |
| Molecular Formula |
C20H25CLN2O5.C6H6O3S
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| Molecular Weight |
567.05
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| Exact Mass |
566.148
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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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| PubChem CID |
60496
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| Appearance |
White to off-white solid powder
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| Density |
1.227g/cm3
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| Boiling Point |
527.2ºC at 760 mmHg
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| Melting Point |
199-201°C
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| Flash Point |
272.6ºC
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| Vapour Pressure |
3.34E-11mmHg at 25°C
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| LogP |
5.309
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
38
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| Complexity |
830
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| Defined Atom Stereocenter Count |
0
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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 |
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