Compound 101

Research use only, not for human use.

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101)?is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101)?is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3; inhibits the desensitization of the G protein-activated inwardly-rectifying potassium current evoked by receptor-saturating concentrations of Met-Enk, DAMGO, endomorphin-2, and morphine in rat and mouse locus coeruleus neurons; produces complete inhibition of DAMGO-induced MOPr phosphorylation at Ser(375), arrestin translocation, and MOPr internalization in HEK 293 cells.

Western Blot Analysis Cell Line:HEK 293 cells stably expressing HA-tagged rat MOPr Concentration:3 μM, 30 μM Incubation Time:Pre-30 minutes Result:Surpressed Ser375 expression completely at a high dose.Western Blot Analysis Cell Line:HEK 293 cells stably expressing HA-tagged rat MOPr Concentration:3 μM, 30 μM Incubation Time:Pre-30 minutes Result:Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression.

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GRK2 inhibitor 101 | Takeda compound 101 | Cmpd101

Others

GRK (GPCRK)

GRK (GPCRK)

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865608-11-3

466.468

C24H21F3N6O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (535.95 mM)

O=C(NCC1=CC=CC=C1C(F)(F)F)C2=CC=CC(NCC3=NN=C(C4=CC=NC=C4)N3C)=C2

3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years