| CAS |
111470-99-6 |
| Chinese Name |
苯磺酸氨氯地平 |
| English Name |
AmLodipine Besylate |
| Synonyms |
苯磺酸氨氯地平;Thioguanine;2-Amino-6-purinethiol;阿罗地平磺酸盐 |
| Molecular Formula |
C20H25ClN2O5·C6H6O3S |
| Molecular Weight |
567.05 |
| Solubility |
Soluble in DMSO |
| Purity |
HPLC≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 1312995-182-4 |
| MDL |
MFCD00887594 |
| SMILES |
O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2Cl)OCC.O=S(C3=CC=CC=C3)(O)=O |
| InChIKey |
ZPBWCRDSRKPIDG-UHFFFAOYSA-N |
| InChI |
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) |
| PubChem CID |
60496 |
| Target Point |
Calcium Channel |
| Passage |
Membrane Transporter&Ion Channel;Neuronal Signaling |
| Background |
It is a long-acting calcium channel inhibitor. |
| Biological Activity |
Amlodipine, a dihydropyridine Ca2 + channel blocker, is reported to inhibit proliferation of human epidermoid carcinoma A431 cells, and specifically attenuates Ca2 + responses evoked by thapsigargin, an inhibitor of endoplasmic reticulum Ca2 +-ATPases.A potential antitumor action for amlodipine in vitro and in vivo, which may be in part mediated by inhibiting Ca2 + influx evoked by the passive depletion of internal Ca2 + stores and by PLC-linked agonist stimulation.[1]. |
| In Vitro |
Amlodipine reduced BrdU incorporation into nucleic acids in serum-starved A431 cells，and the reduction was diminished by uridine 5V_x0002_triphosphate(UTP)，a phospholipase C(PLC)-linked agonist. Fluorometric measurement of intracellular free Ca2 + concentration revealed that amlodipine blunted the UTP-induced Ca2 + release from the internal Ca2 + stores and consequently Ca2 + influx through Ca2 +-permeable channels on the plasma membrane. Although amlodipine alone caused Ca2 + release from thapsigargin-sensitive Ca2 + stores，such an effect was not reproduced by other dihydropyridine Ca2 + channel blockers，including nicardipine and nimodipine，despite their antiproliferative effects in the cells.[1]. |
| In Vivo |
Daily intraperitoneal administration of amlodipine(10 mg/kg)for 20 days into mice bearing A431 xenografts retarded tumor growth and prolonged the survival of mice[1]. |
| Cell Experiment |
Uridine 5V-triphosphate(UTP，20 – 200 AM)was added to serum-starved A431 cells in the absence or presence of amlodipine(20 or 30 AM)，incubated for 48 h，and then labeled with BrdU for 2 h. [1] |
| Animal Experiment |
Three days after tumor inoculation，tumor-bearing mice were randomized to either a control(vehicle)or treated group. Amlodipine for this experiment was dissolved in DMSO to prepare a stock solution(100 mg/ml DMSO)and diluted to 1:100 in phosphate-buffered saline(PBS)，sterilized with 0.2-Am filters on the day of administration. For vehicle treatment，100% DMSO was diluted 1:100 in PBS and sterilized by filtration. Amlodipine(10 mg/kg)or vehicle was administered intraperitoneally(i.p.)once daily for consecutive days. Signs of toxicity and survival of mice were monitored daily. Tumor size was measured by caliper at 2– 3-day intervals.[1] |
| Data Literature Source |
[1]. 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. |
| Unit |
Bottle |
| Specification |
100mg 10mM*1mL in DMSO 1g |
English
中文
Manual Download
