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SML2784

Sigma-Aldrich

CMPD101 hydrochloride

≥98% (HPLC)

Sinônimo(s):

3-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methylamino)-N-(2-(trifluoromethyl)benzyl)benzamide, 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride, Compound 101 hydrochloride, Cpd101 hydrochloride, Takeda101 hydrochloride

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About This Item

Fórmula empírica (Notação de Hill):
C24H21N6OF3 · HCl
Número CAS:
1941168-71-3
Peso molecular:
502.92
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

condição de armazenamento

desiccated

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl

Ações bioquímicas/fisiológicas

CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2), but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

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Yuji Shimizu et al.
Biochemical pharmacology, 140, 105-114 (2017-06-18)
GPR39, a G-protein-coupled receptor activated by zinc, reportedly activates multiple intracellular signaling pathways via Gs, Gq, G12/13, and β-arrestin, but little is known about downregulation of the receptor upon its activation. To our knowledge, this is the first report on
Jesse J DiCello et al.
American journal of physiology. Gastrointestinal and liver physiology, 317(2), G79-G89 (2019-05-16)
Endocytosis is a major mechanism through which cellular signaling by G protein-coupled receptors (GPCRs) is terminated. However, recent studies demonstrate that GPCRs are internalized in an active state and continue to signal from within endosomes, resulting in effects on cellular
Alessandro Cannavo et al.
Frontiers in pharmacology, 10, 888-888 (2019-08-27)
Hyperaldosteronism alters cardiac function, inducing adverse left ventricle (LV) remodeling either via increased fibrosis deposition, mitochondrial dysfunction, or both. These harmful effects are due, at least in part, to the activation of the G protein-coupled receptor kinase 2 (GRK2). In

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