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。


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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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. |
| 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 << |
| 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 |
|
| 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 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
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