| Size | Price | Stock | Qty |
|---|---|---|---|
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| 25g |
|
||
| Other Sizes |
|
Amlodipine maleate (Amvaz; Norvasc), the maleate salt of Amlodipine, is an antihypertensive medication of the dihydropyridine (DHP) class used for lowering blood pressure, angina pectoris and preventing chest pain. It acts as a long-acting L-type calcium channel blocker (CCB).
| ln Vitro |
BrdU incorporation rates in A431 cells were lowered by amlodipine maleate (20–40 μM; 48 hours) to 68.6% and 26.3%, respectively, at doses of 20 and 30 μM [3]. The increase in [Ca2+]i in A431 cells caused by uridine 5'-triphosphate (UTP) was greatly reduced by amlodipine maleate (30 μM) one hour before treatment [3]. In Fluo-3-loaded cells, amlodipine maleate (30 μM) suppresses Thapsigargin-induced store-operated Ca2+ influx [3].
|
|---|---|
| ln Vivo |
In VSMC ATP2B1 KO mice, amlodipine maleate (5 mg/kg/day; subcutaneous injection for 2 weeks) can dramatically lower systolic blood pressure (SBP) [4]. Amlodipine maleate (10 mg/kg; intraperitoneally given once daily for 20 days) can prolong the survival of A431 tumor-bearing mice and considerably delay the formation of tumors [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 |
|
| Additional Infomation |
Amlodipine Maleate is the maleate salt of amlodipine, a synthetic phenylpyridine vasodilator 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. Furthermore, decreased myocardial contractility and dilation of the main coronary and systemic arteries lead to increased blood flow and oxygen delivery to the myocardial tissue and decreases 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 maleate; benazepril hydrochloride (component of). |
| Molecular Formula |
C₂₄H₂₉CLN₂O₉
|
|---|---|
| Molecular Weight |
524.95
|
| Exact Mass |
524.156
|
| CAS # |
88150-47-4
|
| Related CAS # |
Amlodipine;88150-42-9;Amlodipine besylate;111470-99-6;Amlodipine-d4 maleate;2714486-25-4;Amlodipine mesylate;246852-12-0
|
| PubChem CID |
6435922
|
| Appearance |
Light yellow to yellow solid powder
|
| Boiling Point |
527.2ºC at 760 mmHg
|
| Flash Point |
272.6ºC
|
| LogP |
3.007
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
36
|
| Complexity |
766
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN.C(=C\C(=O)O)\C(=O)O
|
| InChi Key |
TZNOWAJJWCGILX-BTJKTKAUSA-N
|
| InChi Code |
1S/C20H25ClN2O5.C4H4O4/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)215-3(6)1-2-4(7)8/h5-8,17,23H,4,9-11,22H2,1-3H31-2H,(H,5,6)(H,7,8)/b2-1-
|
| Chemical Name |
3,5-Pyridinedicarboxylic acid,
2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-,
3-ethyl 5-methyl ester, (+-)-, (Z)-2-butenedioate (1
|
| Synonyms |
Amlodipine (+-)-form maleate, Amvaz
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~120 mg/mL (~228.59 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.71 mg/mL (3.26 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 17.1 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: ≥ 1.71 mg/mL (3.26 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 17.1 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: ≥ 1.71 mg/mL (3.26 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 | 1.9049 mL | 9.5247 mL | 19.0494 mL | |
| 5 mM | 0.3810 mL | 1.9049 mL | 3.8099 mL | |
| 10 mM | 0.1905 mL | 0.9525 mL | 1.9049 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
