SML3946
DFPQ
≥98% (HPLC)
别名:
AP-06-202, N4-Cyclohexyl-N2-(3,4-difluorophenyl)-2,4-quinazolinediamine, N4-Cyclohexyl-N2-(3,4-difluorophenyl)quinazoline-2,4-diamine
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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.
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Michael Ippolito et al.
Proceedings of the National Academy of Sciences of the United States of America, 120(31), e2302668120-e2302668120 (2023-07-25)
Catecholamine-stimulated β2-adrenergic receptor (β2AR) signaling via the canonical Gs-adenylyl cyclase-cAMP-PKA pathway regulates numerous physiological functions, including the therapeutic effects of exogenous β-agonists in the treatment of airway disease. β2AR signaling is tightly regulated by GRKs and β-arrestins, which together promote
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