ChemicalBook Produktkatalog Bio- und Chemieingenieurwesen Inhibitoren Zellzyklus ROCK-Inhibitoren N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Struktur

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

Bezeichnung:N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

CAS-Nr864082-47-3

Englisch Name:N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

CBNumberCB12484722

SummenformelC21H16F4N4O2

Molgewicht432.37

MOL-Datei864082-47-3.mol

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide physikalisch-chemischer Eigenschaften

Siedepunkt	688.4±55.0 °C(Predicted)
Dichte	1.468
storage temp.	Sealed in dry,2-8°C
Löslichkeit	DMSO: ≥10mg/mL
pka	12.10±0.40(Predicted)
Aggregatzustand	powder
Farbe	white to beige
CAS Datenbank	864082-47-3

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
GSK 429286 is a selective Rho-kinase (ROCK) inhibitor.It is orally available and has been shown to dramatically reduce mean arterial pressure in spontaneously hypertensive rats.
Definition
ChEBI: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide is a member of (trifluoromethyl)benzenes.
Biologische Aktivität
gsk429286a is a selective inhibitor of rock1 and rock2 with ic50 value of 14 nm and 63 nm, respectively [1].rho-kinase (rock) is a member of agc (protein kinase a, protein kinase g and protein kinase c) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].gsk429286a is a potent rock inhibitor and has a different activity with the reported rock inhibitor y27632. using gst method, it is shown that gsk429286a treatment (10 μm) increased mypt phosphrylation at thr850 via inhibiting rock which mediated this phosphorylation process [3].in male sprague-dawley rat model with spontaneously hypertensive, oral administration of gsk429286a (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmhg after nearly 2 h treatment [4].
Lager
+4°C
Einzelnachweise
[1]. nichols, r.j., et al., substrate specificity and inhibitors of lrrk2, a protein kinase mutated in parkinson's disease. biochem j, 2009. 424(1): p. 47-60.
[2]. shi, j., et al., distinct roles for rock1 and rock2 in the regulation of cell detachment. cell death dis, 2013. 4: p. e483.
[3]. davis, d.a., et al., increased therapeutic potential of an experimental anti-mitotic inhibitor sb715992 by genistein in pc-3 human prostate cancer cell line. bmc cancer, 2006. 6: p. 22.
[4]. goodman, k.b., et al., development of dihydropyridone indazole amides as selective rho-kinase inhibitors. j med chem, 2007. 50(1): p. 6-9.

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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