GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

PN 200-110 | 4-​(2,​1,​3-​benzoxadiazol-​4-​yl)​-​1,​4-​dihydro-​2,​6-​dimethyl-3,​5-​pyridinedicarboxylic acid 3-​methyl 5-​(1-​methylethyl) ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
In vitro

Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. Isradipine is found to be the most potent derivative in both, in growth cultures (I50 = 20.8 mM) and in vivo oxygen uptake (I50 = 31.1 mM).

In vivo

Isradipine reduces hypoxia-induced activation of calcium dependent xanthine oxidases, monoamine oxidases, cytosolic phospholipase A(2) and cyclooxygenases (COX-2) along with concomitant decrease in free radical generation and cytochrome c release. Isradipine prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. Isradipine (at the dose of 1 mg/kg three times a day) reduces ethanol intake by over 70% in ethanol-preferring rats, the reduction in ethanol intake is compensated by a proportional increase in water consumption and the inhibitory effect persisted throughout the 5 days of treatment. Isradipine significantly reduces the arterial wall collagen contents in both strains, with marked increases in the elastin content in the carotid but not in the aortic wall in spontaneously hypertensive rats. Isradipine suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heroin abuse in mice.
Cell Data

cell lines：MCSF-dependent mouse myeloid M-NFS-60 cell line

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

PN 200-110 | 4-​(2, ​1, ​3-​benzoxadiazol-​4-​yl)​-​1, ​4-​dihydro-​2, ​6-​dimethyl-3, ​5-​pyridinedicarboxylic acid 3-​methyl 5-​(1-​methylethyl) ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.

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

GATING INHIBITOR

Mecanismo de acción

Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Gating inhibitor of Ca v1.4

Nombres e identificadores

• Isómeros SMILES: CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC
• WGK Alemania: 3
• Peso molecular: 371.39
• Reaxy-Rn: 6576633
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6576633&ln=

Objetivos asociados (humanos)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C (4 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)

CACNA1F Tchem Voltage-dependent L-type calcium channel subunit alpha-1F (1 Activities)

Discover Target: CACNA1F

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

Propiedades químicas y físicas

• Punto de fusión (°C): 169 °C