SML3946

DFPQ

≥98% (HPLC)

• Synonym(e): AP-06-202, N4-Cyclohexyl-N2-(3,4-difluorophenyl)-2,4-quinazolinediamine, N4-Cyclohexyl-N2-(3,4-difluorophenyl)quinazoline-2,4-diamine
• Empirische Formel (Hill-System): C₂₀H₂₀F₂N₄
• CAS-Nummer: 911678-60-9
• Molekulargewicht: 354.40
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Quality level: 100

Eigenschaften

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Beschreibung

Biochem/physiol Actions

Gs-biased, β2 subtype-selective adrenergic receptor (AR) negative allosteric modulator (NAM) that inhibits β-arrestin recruitment, but not Gs coupling to β2AR.

DFPQ is a Gs-biased, β2 subtype-selective adrenergic receptor (AR) negative allosteric modulator (NAM) that inhibits β-arrestin recruitment (IC50 = 600 nM; 30-min DFPQ pretreatment prior to 12-min 1 μM ISO induction), but not Gs coupling to β2AR (30-min 10 μM DFPQ pretreatment prior to 10-min 1 μM ISO-induced cAMP production). DFPQ effectively inhibits agonist-induced β2AR phosphorylation (IC50 = 2.6 μM; 30-min DFPQ pretreatment prior to 10-min 1 μM ISO induction) and internalization (100% inhibition by 30-min 10 μM DFPQ prior to 1h 10 μM ISO) and protects against the functional desensitization of β-agonist-mediated regulation in cell and tissue models with minimal effects on β1AR.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable