| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
| Targets |
Amlodipine mesylate targets voltage-dependent L-type calcium channels, which are present in vascular smooth muscle and cardiac muscle. By blocking these channels, it inhibits the influx of calcium ions into cells, leading to vasodilation and reduced peripheral vascular resistance. This mechanism results in a decrease in blood pressure and an increase in oxygen supply to the heart muscle, making it effective for treating hypertension and angina pectoris.
|
|---|---|
| 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].
In vitro, amlodipine mesylate acts as a calcium channel blocker, inhibiting the voltage-dependent L-type calcium channels. Its activity is typically assessed using patch-clamp electrophysiology or calcium flux assays in cell lines expressing these channels. The compound demonstrates potent inhibition of calcium influx, which correlates with its vasodilatory and antihypertensive effects. It has a molecular formula of C21H29ClN2O8S and a molecular weight of 504.98. |
| 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].
In vivo, amlodipine mesylate is an orally active antihypertensive and antianginal agent. It is used for the treatment of hypertension and angina pectoris. Studies have shown that it significantly decreases blood pressure. It can also be used to study hypertension and cancer. Its long half-life supports once-daily dosing, and it is effective in reducing blood pressure over a 24-hour period. |
| Enzyme Assay |
The in vitro receptor binding/functional assay for amlodipine mesylate typically involves measuring its ability to inhibit calcium influx through L-type calcium channels. These assays can be performed using patch-clamp techniques on cells expressing the channels or using fluorescent calcium indicators to measure intracellular calcium levels. The compound's potency (IC50) is determined from concentration-response curves. Its selectivity can be assessed by testing against other ion channels.
|
| Cell Assay |
In vitro cellular assays for amlodipine mesylate assess its effects on calcium signaling and cell function. Vascular smooth muscle cells or cardiac myocytes are treated with the compound, and intracellular calcium levels are measured using fluorescent dyes. Its effects on cell proliferation, migration, or contraction can also be assessed. These assays demonstrate the compound's functional activity as a calcium channel blocker in a relevant cellular context.
|
| 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. In vivo animal studies for amlodipine mesylate have been conducted in various animal models of hypertension. In one study, it was administered subcutaneously via an implanted osmotic pump at a dose of 5 mg/kg/day for 2 weeks, resulting in a significant decrease in blood pressure. Other studies have evaluated its effects on cardiac function, vascular remodeling, and renal protection in hypertensive animal models. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for amlodipine mesylate indicate that it is well-absorbed after oral administration with high bioavailability and a long half-life, supporting once-daily dosing. It is extensively metabolized in the liver and excreted primarily in urine. Its pharmacokinetic profile is similar to that of amlodipine besilate, with a slow onset and long duration of action, making it suitable for chronic use in hypertension and angina.
|
| Toxicity/Toxicokinetics |
Amlodipine mesylate is generally well-tolerated, with a safety profile similar to other dihydropyridine calcium channel blockers. Common adverse effects include peripheral edema, headache, dizziness, and flushing. It should be used with caution in patients with severe hepatic impairment. Its safety has been established through extensive clinical use for hypertension and angina pectoris.
|
| References |
|
| Additional Infomation |
Amlodipine mesylate (CAS 246852-12-0) is an orally active dihydropyridine calcium channel blocker used for the treatment of hypertension and angina. It works by blocking voltage-dependent L-type calcium channels, inhibiting calcium influx. It has a molecular formula of C21H29ClN2O8S and a molecular weight of 504.98. It can also be used to study hypertension and cancer. It is available as a prescription medication.
|
| 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)
|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (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 |
*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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
