Compound 101( GRK2 inhibitor 101 | Takeda compound 101 | Cmpd101 )

Catalog No. M16288 CAS No. 865608-11-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

Compound 101
Note

Research use only, not for human use.
Brief Description

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

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.
In Vitro

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.
In Vivo

——
Synonyms

GRK2 inhibitor 101 | Takeda compound 101 | Cmpd101
Pathway

Others
Target

GRK (GPCRK)
Recptor

GRK (GPCRK)
Research Area

——
Indication

——

CAS Number

865608-11-3
Formula Weight

466.468
Molecular Formula

C24H21F3N6O
Purity

>98% (HPLC)
Solubility

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

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

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

1. Lowe JD, et al. Mol Pharmacol. 2015 Aug;88(2):347-56.

Calculator

molnova catalog