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Amlodipine Besylate

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Chemical Structure| 111470-99-6 同义名 : Amlodipine benzenesulfonate;Amlodipine (besylate)
CAS号 : 111470-99-6
货号 : A804204
分子式 : C26H31ClN2O8S
纯度 : 97%
分子量 : 567.051
MDL号 : MFCD00887594
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(79.36 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(1.76 mM)，配合低频超声助溶
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 6 mg/mL

生物活性
靶点

  • Calcium Channel

    Calcium channel, IC50:1.9 nM
描述 Amlodipine besylate is a long-acting calcium channel blocker. Amlodipine besylate combined with acupoint application of traditional Chinese medicine nursing can effectively reduce the systolic pressure and diastolic pressure of patients, and improve the symptoms and signs of patients, which may be associated with the regulation of the expression of PI3K/AKT (phosphoinositide 3‑kinase /protein kinase B) pathway, so as to regulate the expression of BUN, CRE, UP, BUP and NAG (blood urea nitrogen (BUN), carbapenem‑resistant Enterobacteriaceae (CRE), N‑acetyl‑β‑D‑glucosaminidase (NAG), urine protein (UP) and blood urea protein (BUP))[3]. Perindopril/amlodipine FDC (fixed-dose combination) was significantly more effective in reducing blood pressure (BP) than monotherapy with either of the component drugs, and it appeared to be more effective than an up-titration scheme using valsartan and valsartan/amlodipine[4]. Association of amlodipine besylate and olmesartan medoxomil in fixed-dose combination tablets is effective, safe and well tolerated for the treatment of hypertension[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02058446 Essential Hypertension Phase 4 Completed - Taiwan ... 展开 >> Taichung Veterans General Hospital Taichung, Taiwan, 40705 收起 <<
NCT00591266 Hypertension Phase 3 Completed - -
NCT00627952 Hypertension Phase 3 Completed - Germany ... 展开 >> Clinical Research Center, Department of Nephrology and Hypertension, University of Erlangen-Nurnberg Erlangen, Bavaria, Germany, 91054 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.82mL

1.76mL

0.88mL

17.64mL

3.53mL

1.76mL
参考文献

[1]Lee YJ, Park HH, et al. Amlodipine besylate and amlodipine camsylate prevent cortical neuronal cell death induced by oxidative stress. J Neurochem. 2011 Dec;119(6):1262-70.

[2]Zhou MS, Jaimes EA, et al. Inhibition of oxidative stress and improvement of endothelial function by amlodipine in angiotensin II-infused rats. Am J Hypertens. 2004 Feb;17(2):167-71.

[3]Feng L, Su J, Chi R, Zhu Q, Lv S, Liang W. Effect of amlodipine besylate combined with acupoint application of traditional Chinese medicine nursing on the treatment of renal failure and hypertension by the PI3K/AKT pathway. Int J Mol Med. 2019;43(4):1900‐1910

[4]Shirley M, McCormack PL. Perindopril/amlodipine (Prestalia(®)): a review in hypertension. Am J Cardiovasc Drugs. 2015;15(5):363‐370

[5]Almeida MO, Fernandes C, Pianetti GA, César IC. Simultaneous Quantitation of Amlodipine Besylate and Olmesartan Medoxomil in Fixed-Dose Combination Tablets: HPLC-DAD Versus UHPLC-DAD. J Chromatogr Sci. 2018;56(4):344‐350