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Amlodipine Besylate/苯磺酸氨氯地平 {[allProObj[0].p_purity_real_show]}

货号:A804204 同义名: Amlodipine benzenesulfonate; Amlodipine(benzenesulfonate)

Amlodipine Besylate是一种长效钙通道阻滞剂,用于降低血压和预防胸痛。

Amlodipine Besylate/苯磺酸氨氯地平 化学结构 CAS号:111470-99-6
Amlodipine Besylate/苯磺酸氨氯地平 化学结构
CAS号:111470-99-6
Amlodipine Besylate/苯磺酸氨氯地平 3D分子结构
CAS号:111470-99-6
Amlodipine Besylate/苯磺酸氨氯地平 化学结构 CAS号:111470-99-6
Amlodipine Besylate/苯磺酸氨氯地平 3D分子结构 CAS号:111470-99-6
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Amlodipine Besylate/苯磺酸氨氯地平 纯度/质量文件 产品仅供科研

货号:A804204 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone HCl 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

p38 MAPK,ERK,ROS 99%+
Fasudil HCl Rho,PKA 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 99%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 99%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 98%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

95%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 99%
Cinepazide Maleate 99% (HPLC)
Terfenadine 98%
YM-58483 99%+
Amiloride HCl 98%
Ranolazine 98%
Praeruptorin A Akt,p38 MAPK 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Amlodipine Besylate/苯磺酸氨氯地平 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].

Amlodipine Besylate/苯磺酸氨氯地平 细胞实验

Cell Line
Concentration Treated Time Description References
Rat liver microsomes 1 µM 0, 1, 3, 5, 15, 30, 60 minutes To investigate the effect of curcumin on the metabolic stability of amlodipine. Results showed that curcumin significantly prolonged the half-life of amlodipine (from 34.23 ± 3.33 min to 44.15 ± 4.12 min) and decreased its intrinsic clearance rate (from 40.49 ± 3.26 μL/min/mg protein to 31.39 ± 2.78 μL/min/mg protein). Pharm Biol. 2020 Dec;58(1):465-468.
HL-1 cells 5 µM 1 hour Observe the distribution and accumulation of AML in live cells Molecules. 2021 May 18;26(10):2997.
A7r5 cells 5 µM 1 hour Observe the distribution and accumulation of AML in live cells Molecules. 2021 May 18;26(10):2997.
HEK-293 CaV1.2 cells 300 nM 15 minutes Observe the distribution and accumulation of AML in live cells Molecules. 2021 May 18;26(10):2997.
Human aortic artery-derived VSMCs 5 µM 24 hours To investigate the effect of Amlodipine on miR-21 promoter activity, results showed that Amlodipine enhanced miR-21 promoter activity Br J Pharmacol. 2019 Jul;176(13):2306-2320.
Rat aortic artery-derived VSMCs 5 µM 24 hours To investigate the effect of Amlodipine on miR-21 expression, results showed that Amlodipine induced miR-21 overexpression Br J Pharmacol. 2019 Jul;176(13):2306-2320.
MGC803 cells 0, 5, 10, 20 µM 24, 48, 72 hours To evaluate the effect of Amlodipine on cell proliferation, results showed that Amlodipine inhibited GC cell proliferation in a dose-dependent manner. Funct Integr Genomics. 2024 Apr 18;24(3):77.
HGC27 cells 0, 5, 10, 20 µM 24, 48, 72 hours To evaluate the effect of Amlodipine on cell proliferation, results showed that Amlodipine inhibited GC cell proliferation in a dose-dependent manner. Funct Integr Genomics. 2024 Apr 18;24(3):77.
TE-1 4-10 μg/mL 24-72 hours To evaluate the inhibitory effect of amlodipine on the proliferation of esophageal cancer cells, the results showed that amlodipine decreased cell viability in a dose- and time-dependent manner. World J Gastroenterol. 2024 Jan 28;30(4):367-380.
SKGT-4 4-10 μg/mL 24-72 hours To evaluate the inhibitory effect of amlodipine on the proliferation of esophageal cancer cells, the results showed that amlodipine decreased cell viability in a dose- and time-dependent manner. World J Gastroenterol. 2024 Jan 28;30(4):367-380.
Eca109 4-10 μg/mL 24-72 hours To evaluate the inhibitory effect of amlodipine on the proliferation of esophageal cancer cells, the results showed that amlodipine decreased cell viability in a dose- and time-dependent manner. World J Gastroenterol. 2024 Jan 28;30(4):367-380.
KYSE-450 4-10 μg/mL 24-72 hours To evaluate the inhibitory effect of amlodipine on the proliferation of esophageal cancer cells, the results showed that amlodipine decreased cell viability in a dose- and time-dependent manner. World J Gastroenterol. 2024 Jan 28;30(4):367-380.
Rat liver microsomes 1 µM 60 minutes To investigate the inhibitory effects of triptolide on the metabolic stability of amlodipine. Results showed that triptolide pretreatment prolonged the metabolic half-life of amlodipine from 22.5±4.26 to 36.8±6.37 minutes. Pharm Biol. 2018 Dec;56(1):132-137.
H9c2 cells 2.75 µM 72 hours To evaluate the toxicity of Amlodipine on H9c2 cells and its anti-T. cruzi activity. Results showed that Amlodipine exhibited anti-T. cruzi activity in the micromolar range with moderate toxicity to host cells. Antimicrob Agents Chemother. 2020 Jul 22;64(8):e02497-19.

Amlodipine Besylate/苯磺酸氨氯地平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
ApoE-/- mice Atherosclerosis model Chow supplemented 1.5 mg/kg/day Daily administration for 25 weeks To evaluate the effects of amlodipine on atherosclerotic lesion size and composition. Results showed that amlodipine monotherapy did not significantly reduce lesion size, but a trend toward decrease was observed. Additionally, significantly thicker fibrous caps were found in the amlodipine-treated group. Drug Des Devel Ther. 2015 Jul 29;9:3935-42
Female Swiss mice T. cruzi Y strain infection model Oral 10 mg/kg Once daily for 5 consecutive days To evaluate the efficacy of Amlodipine in combination with ravuconazole in T. cruzi-infected mice. Results showed that Amlodipine alone lacked trypanocidal activity but significantly enhanced the antiparasitic effect of ravuconazole when used in combination. Antimicrob Agents Chemother. 2020 Jul 22;64(8):e02497-19.
NKG mice Subcutaneous xenograft model Oral 10 mg/kg/day Once daily for 28 days To evaluate the effect of Amlodipine on tumor growth in vivo, results showed that Amlodipine significantly reduced tumor growth and volume in SYT4-OE group mice. Funct Integr Genomics. 2024 Apr 18;24(3):77.
Mice Hypertensive BPH/2J and normotensive BPN/3J mice Drinking water 10 mg/kg/day Daily administration until 12 months of age To investigate the effect of amlodipine on BP, BPv, cognitive function, BBB integrity and neuroinflammation in aged hypertensive mice. Results showed that amlodipine normalized SBP and BPv, attenuated short-term memory impairment, and partly reduced microglial inflammatory phenotype. J Hypertens. 2023 Jul 1;41(7):1159-1167
BALB/c nude mice Esophageal cancer xenograft model Oral gavage 13 mg/kg/day Once daily for 15 days To evaluate the inhibitory effect of amlodipine on esophageal cancer growth in vivo, the results showed that amlodipine significantly inhibited tumor growth with a tumor inhibition rate of 30.95%. World J Gastroenterol. 2024 Jan 28;30(4):367-380.
Spontaneously hypertensive rats Spontaneously hypertensive rat model Oral 2 mg/kg/day Once daily for 10 weeks To investigate the effect of Amlodipine on miR-21 expression and vascular smooth muscle cell differentiation, results showed that Amlodipine induced miR-21 overexpression and promoted vascular smooth muscle cell differentiation Br J Pharmacol. 2019 Jul;176(13):2306-2320.

Amlodipine Besylate/苯磺酸氨氯地平 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 <<

Amlodipine Besylate/苯磺酸氨氯地平 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

Amlodipine Besylate/苯磺酸氨氯地平 实验方案

计算器
存储液制备 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

Amlodipine Besylate/苯磺酸氨氯地平 技术信息

CAS号111470-99-6
分子式C26H31ClN2O8S
分子量 567.05
SMILES Code O=C(OC)C1=C(NC(=C(C(=O)OCC)C1C=2C=CC=CC2Cl)COCCN)C.O=S(=O)(O)C=1C=CC=CC1
MDL No. MFCD00887594
别名 Amlodipine benzenesulfonate; Amlodipine(benzenesulfonate)
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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