Cilnidipine (FRC-8653) - Moligand™, 10mM in DMSO , Voltage-gated L-type calcium channel blocker, CAS No.132203-70-4, Voltage-gated L-type calcium channel blocker

CAS: 132203-70-4 Cat. No.: C407809 Peso molecular: 492.52 Número EC: 634-350-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

3-cinnamyl 5-(2-methoxyethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Cilnidipine (FRC-8653) Cilnidipine (FRC-8653) is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
In vitro

Cilnidipine (10 mM) suppresses the elevation of the ratio induced by 40 mM KCl, and this suppression is effectively inhibited after the treatment with omega-conotoxin GVIA.

In vivo

Cilnidipine reduces Ca(2+) influx via N-type Ca(2+) channels after NMDA receptors activation and then protects neurons against ischemia-reperfusion injury in the rat retina in vivo. Cilnidipine\xa0significantly prevents the increase in desmin staining and restores the glomerular podocin and nephrin expression compared with amlodipine in spontaneously hypertensive rat/ND mcr-cp (SHR/ND).\xa0Cilnidipine also prevents the increase in renal angiotensin II content, the expression and membrane translocation of NADPH oxidase subunits and dihydroethidium staining in SHR/ND. Cilnidipine (30 mg/kg/d as food admix) treatment suppresses the increase in systolic blood pressure in\xa0Dahl\xa0salt-sensitive rats.\xa0Cilnidipine inhibits the increase in blood urea nitrogen and decrease in creatinine clearance as well as progression of glomerular sclerosis. Cilnidipine\xa0reduces plasma norepinephrine level and plasma rennin activity compared with vehicle-treated\xa0Dahl S rats.\xa0 Cilnidipine suppresses the pressor response induced by sympathetic nerve stimulation and angiotensin II in pithed rats. Cilnidipine or omega-conotoxin MVIIA decreases mean blood pressure, but slightly increases heart rate in anesthetized rats. Cilnidipine can affect sympathetic N-type Ca(2+) channels in addition to vascular L-type Ca(2+) channels in antihypertensive doses in the rat in vivo.\xa0
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

3-cinnamyl 5-(2-methoxyethyl) 2, 6-dimethyl-4-(3-nitrophenyl)-1, 4-dihydropyridine-3, 5-dicarboxylate

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Cilnidipine (FRC-8653) is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.

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

BLOCKER, CHANNEL BLOCKER

Mecanismo de acción

Voltage-gated L-type calcium channel blocker

Nombres e identificadores

• Isómeros SMILES: CC1=C(C(C(=C(N1)C)C(=O)OC/C=C/C2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCOC
• WGK Alemania: 3
• RTECS: US7975550
• Peso molecular: 492.52
• Reaxy-Rn: 36145545
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36145545&ln=

Objetivos asociados (humanos)

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

Discover Target: CACNA1C

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

CACNA1B Tclin Voltage-dependent N-type calcium channel subunit alpha-1B (2 Activities)

Discover Target: CACNA1B

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

Propiedades químicas y físicas

• Punto de fusión (°C): 110 °C