GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

CGH-869 | 4-​(2,​3-​dichlorophenyl)​-​1,​4-​dihydro-​2,​6-​dimethyl-3,​5-​pyridinedicarboxylic acid-3-​ethyl 5-​methyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Felodipine Felodipine (CGH-869) is a selective L-type Ca 2+ channel blocker with IC50 of 0.15 nM.

In vitro

Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM). Felodipine significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes. Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM. Felodipine at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells. Felodipine (10 μM) reduces nuclear translocation of p42/44 mitogen-activated protein kinase and Elk-1 activation stimulated by PDGF-BB, leading to the inhibition of human SMC proliferation. Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM.

In vivo

Oral administration of Felodipine significantly reduces the average blood pressure (BP) in rats with 5/6 renal ablation, but causes additional impairment of the already impaired renal autoregulation. Administration of Felodipine significantly reduces systolic blood pressure (SBP), serum insulin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by blocking NF-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response.

Cell Data

cell lines：MT-4

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

CGH-869 | 4-​(2, ​3-​dichlorophenyl)​-​1, ​4-​dihydro-​2, ​6-​dimethyl-3, ​5-​pyridinedicarboxylic acid-3-​ethyl 5-​methyl ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Selective L-type Ca 2+ channel blocker. Selective over N-, R-, P/Q- and T-type channels. Displays high vascular selectivity and shows antihypertensive effects in vivo. Orally active.

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

ACTIVATOR

Mecanismo de acción

Activator of CFTR

Nombres e identificadores

• Isómeros SMILES: CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
• WGK Alemania: 3
• RTECS: US7968700
• CAS alternativo: 86189-69-7
• Peso molecular: 384.25
• Reaxy-Rn: 4331472
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4331472&ln=

Objetivos asociados (humanos)

CFTR Tclin Cystic fibrosis transmembrane conductance regulator (1 Activities)

Discover Target: CFTR

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

Propiedades químicas y físicas

• Punto de fusión (°C): 142.0°C-146.0°C

Referencias

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo.  (2023)  Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,      [PMID:] [10.1016/j.jfca.2023.105825]

2. Yin Xuezhi, Pan Hao, Liu Hongfei.  (2019)  A Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray.  AAPS PHARMSCITECH,  20  (7): (1-8).  [PMID:31407104] [10.1208/s12249-019-1495-8]