Amlodipine - Moligand™, 10mM in DMSO , Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Allosteric modulator of P2X4, CAS No.88150-42-9, Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Allosteric modulator of P2X4

CAS: 88150-42-9 Cat. No.: A408387 Peso molecular: 408.88 Número EC: 618-119-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

UK-48340 | 2-​[(2-​aminoethoxy)​methyl]​-​4-​(2-​chlorophenyl)​-​1,​4-​dihydro-​6-​methyl-​3,​5-​pyridinedicarboxylic acid 3-​ethyl 5-​methyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Amlodipine Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
In vitro

Amlodipine causes a dose-dependent increase in nitrite production. Amlodipine also increases nitrite production in large coronary arteries and in aorta. Amlodipine is attributed to distinct membrane physico-chemical interactions. Amlodipine contributes to distinct membrane biophysical interactions that lead to potent lipid antioxidant effects, independent of calcium channel modulation. Amlodipine increases plaque smooth muscle cell content (P<0.05), whereas atenolol decreases plaque inflammation. Amlodipine attenuates intracellular neuronal Ca²⁺ increases elicited by KCl depolarization but does not affect Ca²⁺ changes triggered by N-methyl-D-aspartate receptor activation. Amlodipine also inhibits free radical-induced damage to lipid constituents of the membrane in a dose-dependent manner, independent of Ca²⁺ channel modulation.

In vivo

Amlodipine results in regression of cardiovascular hypertrophy and amelioration of endothelial dysfunction in spontaneously hypertensive rats. Amlodipine significantly reduces aortic hypertrophy, endothelial dysfunction, LOX-1 expression, aortic O(2)(-) and ONOO(-) production, and plasma free 8-F(2)alpha-isoprostane levels in Ang II-infused rats. Amlodipine has antihypertensive and antioxidant activity in vivo, which effectively inhibits many of the oxidative stress-dependent mechanisms involved in Ang II-mediated cardiovascular injury.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥95%

Specifications

Sinónimos

UK-48340 | 2-​[(2-​aminoethoxy)​methyl]​-​4-​(2-​chlorophenyl)​-​1, ​4-​dihydro-​6-​methyl-​3, ​5-​pyridinedicarboxylic acid 3-​ethyl 5-​methyl ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ALLOSTERIC MODULATOR, GATING INHIBITOR

Mecanismo de acción

Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Allosteric modulator of P2X4

Nombres e identificadores

• Isómeros SMILES: CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN
• Peso molecular: 408.88
• Reaxy-Rn: 3570229
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3570229&ln=

Objetivos asociados (humanos)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C (2 Activities)

Discover Target: CACNA1C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CACNA1D Tclin Voltage-dependent L-type calcium channel subunit alpha-1D (1 Activities)

Discover Target: CACNA1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNK2 Tclin Potassium channel subfamily K member 2 (1 Activities)

Discover Target: KCNK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 178-179 ºC

Referencias

1. Chehao Lee, Guang Xin, Fan Li, Chengyu Wan, Xiuxian Yu, Lijuan Feng, Ao Wen, Yu Cao, Wen Huang.  (2023)  Calcium/P53/Ninjurin 1 Signaling Mediates Plasma Membrane Rupture of Acinar Cells in Severe Acute Pancreatitis.  INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,  24  (14): (11554).  [PMID:37511311] [10.3390/ijms241411554]

2. Zhimin Gong, Gaobo Wang, Shuai Shao, Mengjie Wang, Kun Lu, Shixiang Gao.  (2021)  Co-degradation of coexisting pollutants methylparaben (mediators) and amlodipine in enzyme-mediator systems: Insight into the mediating mechanism.  JOURNAL OF HAZARDOUS MATERIALS,      [PMID:34523479] [10.1016/j.jhazmat.2021.127112]

3. Zhu-Jun Zhong, Zhong-Ping Yao, Zi-Qi Shi, Yang-Dan Liu, Li-Fang Liu, Gui-Zhong Xin.  (2021)  Measurement of Intracellular Nitric Oxide with a Quantitative Mass Spectrometry Probe Approach.  ANALYTICAL CHEMISTRY,      [PMID:34107211] [10.1021/acs.analchem.1c01259]

4. Yujie Zhang, Hui Zhong, Shouyong Zhou, Haifeng Han, Mingliang Zhang, Hongdeng Qiu.  (2021)  A docosyl-terminated polyamine amphiphile-bonded stationary phase for multimodal separations in liquid chromatography.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:33735643] [10.1016/j.chroma.2021.462045]

5. Lelin Zeng, Qin Yi, Qian Liu, Kewen Tang, Bart Van der Bruggen.  (2020)  Development of a new method and device for chiral drug enrichment and enantioseparation: Multiple-phase extraction and in situ coupling of crystallization.  SEPARATION AND PURIFICATION TECHNOLOGY,      [PMID:] [10.1016/j.seppur.2020.117884]

6. Lelin Zeng, Qian Liu, Bart Van der Bruggen, Kewen Tang, Xiang Yi, Guoxiang Wang.  (2020)  An integrated separation process for recovery and enantioseparation of amlodipine from wastewater: Supported liquid membrane-aqueous/organic phase crystallization.  SEPARATION AND PURIFICATION TECHNOLOGY,      [PMID:] [10.1016/j.seppur.2020.117121]

7. Shuai Shao, Li Qian, Xin Zhan, Mengjie Wang, Kun Lu, Jianbiao Peng, Dong Miao, Shixiang Gao.  (2019)  Transformation and toxicity evolution of amlodipine mediated by cobalt ferrite activated peroxymonosulfate: Effect of oxidant concentration.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2019.123005]

8. Ruike Song, Yanxia Li, Yiting Chen, Zhenli Qiu, Lu Huang.  (2023)  Chiral covalent organic framework incorporated organic polymer monolithic capillary column for enantioseparations.  JOURNAL OF SEPARATION SCIENCE,  46  (8): (2201039).  [PMID:36750206] [10.1002/jssc.202201039]

9. Shi Ruirui, Wang Chao, Zhu Mingyue, Xie Chen, Cui Wenyu, Zhou Qing.  (2025)  A smartphone-assisted colorimetric paper sensor based on MnO2 nanozymes as oxidase mimetics for rapid evaluation of total antioxidant capacity in foods.  MICROCHIMICA ACTA,  192  (7): (1-10).  [PMID:40500337] [10.1007/s00604-025-07277-9]