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SML0774

Sigma-Aldrich

SR 3677

≥98% (HPLC)

Sinônimo(s):

N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide., SR-3677, SR3677

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About This Item

Fórmula empírica (Notação de Hill):
C22H24N4O4
Número CAS:
Peso molecular:
408.45
Código UNSPSC:
12352200

Ensaio

≥98% (HPLC)

forma

powder

cor

white to light brown

solubilidade

DMSO: 15 mg/mL, clear

temperatura de armazenamento

2-8°C

InChI

1S/C22H24N4O4/c1-26(2)9-10-28-20-11-15(16-12-23-24-13-16)7-8-17(20)25-22(27)21-14-29-18-5-3-4-6-19(18)30-21/h3-8,11-13,21H,9-10,14H2,1-2H3,(H,23,24)(H,25,27)

chave InChI

OQWZIAVXCYIZNN-UHFFFAOYSA-N

Aplicação

SR 3677 has been used as Rho-associated kinase (ROCK) inhibitor in cardiac reprogramming.

Ações bioquímicas/fisiológicas

SR-3677 is a very potent, selective ROCK inhibitor, with higher potency against ROCK II (IC50 = 3 nM) than ROCK I (IC50 = 56 nM). In a kinase screening panel, SR-3677 was shown to only have activity against three other kinases (PKA, MRCK and Akt1) all with IC50 values over 1 μM. The compound has nM potency in cell based assays, and is efficacious in an ex-vivo model for increasing aqueous humor outflow in porcine eyes.
SR3677 decreases amyloid precursor protein (sAPPβ) and amyloid-β (Aβ) in a dose-dependent manner. In 5XFAD mouse brain, SR3677 represses the enzymatic activity of β-site APP cleaving enzyme 1 (BACE1). SR3677 has the ability to change the endocytic supply of BACE1 and induce APP traffic to lysosomes.

Características e benefícios

This compound is featured on the PKA & PKG and PKB/Akt pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictogramas

Exclamation mark

Palavra indicadora

Warning

Frases de perigo

Classificações de perigo

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Órgãos-alvo

Respiratory system

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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Jeremy H Herskowitz et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 33(49), 19086-19098 (2013-12-07)
Alzheimer's disease (AD) is the leading cause of dementia and has no cure. Genetic, cell biological, and biochemical studies suggest that reducing amyloid-β (Aβ) production may serve as a rational therapeutic avenue to delay or prevent AD progression. Inhibition of
Yuanbiao Zhao et al.
Nature communications, 6, 8243-8243 (2015-09-12)
Direct reprogramming of fibroblasts into cardiomyocytes by forced expression of cardiomyogenic factors, GMT (GATA4, Mef2C, Tbx5) or GHMT (GATA4, Hand2, Mef2C, Tbx5), has recently been demonstrated, suggesting a novel therapeutic strategy for cardiac repair. However, current approaches are inefficient. Here

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