Bufuralol

• UNSPSC Description:

  Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate[1][2][3][4].

• Target Antigen:

  Adrenergic Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Neuronal Signaling

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Endocrinology; Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/bufuralol.html

• Purity:

  99.17

• Solubility:

  DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

  CCC1=CC=CC2=C1OC(C(O)CNC(C)(C)C)=C2

• Molecular Weight:

  261.36

• References & Citations:

  [1]T H Pringle, et al. Pharmacodynamic and pharmacokinetic studies on bufuralol in man. Br J Clin Pharmacol. 1986 Nov;22(5):527-34.|[2]Jie Cai, et al. Effects of 22 Novel CYP2D6 Variants Found in the Chinese Population on the Bufuralol and Dextromethorphan Metabolisms In Vitro. Basic Clin Pharmacol Toxicol. 2016 Mar;118(3):190-9.|[3]Sarah M Glass, et al. CYP2D6 Allelic Variants *34, *17-2, *17-3, and *53 and a Thr309Ala Mutant Display Altered Kinetics and NADPH Coupling in Metabolism of Bufuralol and Dextromethorphan and Altered Susceptibility to Inactivation by SCH 66712. Drug Metab Dispos. 2018 Aug;46(8):1106-1117.|[4]T Prueksaritanont, et al. (+)-bufuralol 1'-hydroxylation activity in human and rhesus monkey intestine and liver. Biochem Pharmacol. 1995 Oct 26;50(9):1521-5.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture and light)

• Clinical Information:

  No Development Reported

• CAS Number:

  54340-62-4