Isradipine - Moligand™, 10mM in DMSO , Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Gating inhibitor of Ca v1.4, CAS No.75695-93-1, Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3;Gating inhibitor of Ca v1.4

CAS: 75695-93-1 Cat. No.: I408783 Molecular Weight: 371.39 EC Number: 630-420-5

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

Overview

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

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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

GATING INHIBITOR

Mechanism of action

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

Names and Identifiers

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

Associated Targets(Human)

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)

Chemical and Physical Properties

• Melt Point(°C): 169 °C