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CAS
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111470-99-6
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中文名称
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苯磺酸氨氯地平
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英文名称
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AmLodipine Besylate
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别名
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Amlodin; Norvasc
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纯度
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HPLC≥98%
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分子式
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C20H25ClN2O5·C6H6O3S
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分子量
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567.05
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外观（性状）
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White to off-white Solid
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储存条件
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Powder : 2-8℃, 2 years; In solvent(母液): -20℃, 1 month; -80℃, 6 months
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溶解性
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Soluble in DMSO
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EC
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EINECS 1312995-182-4
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MDL
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MFCD00887594
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InChIKey
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ZPBWCRDSRKPIDG-UHFFFAOYSA-N
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InChI
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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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PubChem CID
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60496
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SMILES
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O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2Cl)OCC.O=S(C3=CC=CC=C3)(O)=O
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描述
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是长效钙离子通道抑制剂。(It is a long-acting calcium channel inhibitor.)
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靶点
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Calcium Channel
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通路
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Membrane Transporter&Ion Channel;Neuronal Signaling
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生物活性
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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].
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In Vitro
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Amlodipine reduced BrdU incorporation into nucleic acids in serum-starved A431 cells, and the reduction was diminished by uridine 5V_x005ftriphosphate (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].
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In Vivo
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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].
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细胞实验
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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]
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动物实验
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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, 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]
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数据来源文献
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[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.
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规格
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100mg 10mM*1mL (in DMSO) 1g
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单位
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瓶
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