Amlodipine mesylate (Amlodis; Amlor, Coroval; Lipinox; Norvasc; Amvaz), the mesylate salt of Amlodipine, is an approved anti-hypertensive drug of the dihydropyridine (DHP) class used for lowering blood pressure. It acts as a long-acting L-type calcium channel blocker (CCB).
Physicochemical Properties
| Molecular Formula | C21H29CLN2O8S |
| Molecular Weight | 504.97 |
| Exact Mass | 504.133 |
| CAS # | 246852-12-0 |
| Related CAS # | Amlodipine;88150-42-9;Amlodipine maleate;88150-47-4;Amlodipine besylate;111470-99-6 |
| PubChem CID | 10300874 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 3.88 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 10 |
| Heavy Atom Count | 33 |
| Complexity | 739 |
| Defined Atom Stereocenter Count | 0 |
| 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(C([H])([H])[H])(=O)(=O)O[H] |
| InChi Key | MUVFCHUBATVFPP-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C20H25ClN2O5.CH4O3S/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)211-5(2,3)4/h5-8,17,23H,4,9-11,22H2,1-3H31H3,(H,2,3,4) |
| Chemical Name | 3-ethyl 5-methyl 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate methanesulfonate |
| Synonyms | Amlodis Amlor, Coroval Lipinox NorvascAmvaz |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| ln Vitro | BrdU incorporation rates in A431 cells were lowered by amlodipine mesylate (20–40 μM; 48 hours) to 68.6% and 26.3%, respectively, at doses of 20 and 30 μM [3]. Amlodipine mesylate (30 μM; 1 hour pretreatment) dramatically reduced the rise in [Ca2+]i in A431 cells caused by uridine 5'-triphosphate (UTP) [3]. In Fluo-3-loaded cells, amlodipine mesylate (30 μM) suppresses Thapsigargin-induced store-operated Ca2+ influx [3]. |
| ln Vivo | Amlodipine mesylate (5 mg/kg/day; subcutaneous injection for 2 weeks) can dramatically reduce systolic blood pressure (SBP) in VSMC ATP2B1 KO mice [4]. Amlodipine mesylate (10 mg/kg; intraperitoneally given once daily for 20 days) can considerably decrease tumor growth and lengthen the longevity of A431 tumor-bearing mice [3]. |
| Animal Protocol |
Animal/Disease Models: ATP2B1loxP/loxP mice [4] Doses: 5 mg/kg/day Route of Administration: subcutaneously (sc) (sc) implanted osmotic pump for 2 weeks Experimental Results: Dramatically lowered blood pressure. |
| References |
[1]. Amlodipine. [2]. 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]. 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]. 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. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9803 mL | 9.9016 mL | 19.8032 mL | |
| 5 mM | 0.3961 mL | 1.9803 mL | 3.9606 mL | |
| 10 mM | 0.1980 mL | 0.9902 mL | 1.9803 mL |