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SML0774

Sigma-Aldrich

SR 3677

≥98% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C22H24N4O4
Numero CAS:
1072959-67-1
Peso molecolare:
408.45
Codice UNSPSC:
12352200

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to light brown

Solubilità

DMSO: 15 mg/mL, clear

Temperatura di conservazione

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)
OQWZIAVXCYIZNN-UHFFFAOYSA-N

Applicazioni

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

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Pittogrammi

Exclamation mark
GHS07

Avvertenze

Warning

Indicazioni di pericolo

H315,H319,H335

Classi di pericolo

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

Organi bersaglio

Respiratory system

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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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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