Nisoldipine - Moligand™, 10mM in DMSO , Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3, CAS No.63675-72-9, Gating inhibitor of Ca v1.2;Gating inhibitor of Ca v1.3

CAS: 63675-72-9 Cat. No.: N408419 Summenformel: C₂₀H₂₄N₂O₆ Molekulargewicht: 388.41 EG-Nummer: 264-407-7

QUALITÄT & REINHEIT Moligand™, 10mM in DMSO

Synonyms

BAY K 5552 | 1,​4-​dihydro-​2,​6-​dimethyl-​4-​(2-​nitrophenyl)​-​3,​5-​pyridinedicarboxylic acid-3-​methyl 5-​(2-​methylpropyl) ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Nisoldipine Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Ca v 1.2 with IC50 of 10 nM.
In vitro

Nisoldipine is a potent blocker of L-type calcium channels. Nisoldipine binds directly to inactive calcium channels stabilizing their inactive conformation Similar to other DHP CCBs. Nisoldipine displays selectivity for arterial smooth muscle cells due to great number of inactive channels and the α1 subunit of the channel. Nisoldipine is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca²⁺ channels, which inhibits I_Kr (rapidly activating delayed-rectifier K⁺ current) with IC50 of 23 μM, and IKs (slowly activating delayed-rectifier K⁺ current)with IC50 of 40 μM in guinea-pig ventricular myocytes. Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen. This is tested by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC1₃-ADP).

In vivo

Nisoldipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. This results in vasodilation and an overall decrease in blood pressure, based on which Nisoldipine is used to treat mild to moderate essential hypertension, chronic stable angina and Prinzmetal\'s variant angina. Nisoldipine shows some ability in patients with Timothy syndrome having Ca_v1.2 missense mutation G406R with IC50 of 267 nM, which is helpful to treat TS.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO, final concentration 10-100 μM

Incubation Time：8-10 minutes

Powder Purity:≥99%

Spezifikationen

Synonyme

BAY K 5552 | 1,​4-​dihydro-​2,​6-​dimethyl-​4-​(2-​nitrophenyl)​-​3,​5-​pyridinedicarboxylic acid-3-​methyl 5-​(2-​methylpropyl) ester

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Ca_v1.2 with IC50 of 10 nM.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

GATING INHIBITOR

Mechanismus der Wirkung

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

Namen und Kennungen

Isomere SMILES

CC1=C(C(C(=C(N1)C)C(=O)OCC(C)C)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC

WGK Deutschland

3

RTECS

US7975600

Molekulargewicht

388.41

Reaxy-Rn

454188

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=454188&ln=

Zugehörige Ziele (menschlich)

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

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

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)

Chemische und physikalische Eigenschaften

• Schmelzpunkt (°C): 153 °C

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 63675-72-9, the molecular formula is C20H24N2O6, and the molecular weight is 388.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.