Acebutolol HCl - 10mM in DMSO , Beta-1 adrenergic receptor antagonist, CAS No.34381-68-5, Beta-1 adrenergic receptor antagonist

CAS: 34381-68-5 Cat. No.: A408001 Summenformel: C₁₈H₂₈N₂O₄·HCl Molekulargewicht: 372.89 EG-Nummer: 251-980-3

GRADE & PURITY 10mM in DMSO

Synonyms

Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-, hydrochloride (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Acebutolol is aβ-adrenergic receptorsantagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
In vitro

Acebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. Acebutolol produces a concentration-dependent inhibition of ¹²⁵I-labeled CYP binding to human fat cell membranes and are able to completely displace all specifically bound radioligand. Acebutolol totally inhibits lipolytic activity initiated by 1 μM isoproterenol. Acebutolol is a cardioselective antagonist possessing low lipid solubility. Acebutolol, which does not bind to LDL, shows a stronger inhibiting effect on the intracellular accumulation of cholesterol esters in J774 macrophages than alprenolol and oxprenolol which bind to LDL.

In vivo

Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9\u2009mL/min/kg, the volume of distribution of 9.6\u2009L/kg, and an elimination half-life of 1.8\u2009hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5\u2009mL/min/kg, the volume of distribution of 9.5\u2009L/kg, and an elimination half-life of 2.3\u2009hours. Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats.
Cell Data

cell lines：RS4;11, MV4;11, and OC1-AML5

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyme

Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-, hydrochloride (1:1)

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

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

Aktionsart

ANTAGONIST

Mechanismus der Wirkung

Beta-1 adrenergic receptor antagonist

Namen und Kennungen

Isomere SMILES

CCCC(=O)NC1=CC(=C(C=C1)OCC(CNC(C)C)O)C(=O)C.Cl

WGK Deutschland

3

RTECS

ES5235000

Molekulargewicht

372.89

Reaxy-Rn

6080568

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6080568&ln=

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro Water: 1 mg/mL (6.05 mM); DMSO: Insoluble; Ethanol: Insoluble
• Schmelzpunkt (°C): 143-145°C