A 804598 Struktur

A 804598

Bezeichnung:A 804598

CAS-Nr1125758-85-1

Englisch Name:A 804598

CBNumberCB82602998

SummenformelC19H17N5

Molgewicht315.37

MOL-Datei1125758-85-1.mol

A 804598 physikalisch-chemischer Eigenschaften

Siedepunkt	498.0±47.0 °C(Predicted)
Dichte	1.17±0.1 g/cm3(Predicted)
storage temp.	Keep in dark place,Sealed in dry,2-8°C
Löslichkeit	DMSO: soluble10mg/mL, clear
pka	4.52±0.12(Predicted)
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

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

Gefahreninformationscode (GHS)

A 804598 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
A 804598 is a P2X7 antagonist.
Biologische Aktivität
a 804598 is a potent and selective antagonist of p2x7 receptor with ic50 values of 8.9, 9.9 and 10.9 nm for mouse, rat and human p2x7 receptors, respectively [1].p2x purinoceptor 7 (p2x7 receptor) is a purinoceptor and is activated by high concentrations of atp. p2x7 receptor plays an important role in atp-mediated cell death, inflammation and regulation of receptor trafficking.a 804598 is a potent and selective p2x7 receptor antagonist. in differentiated thp-1 cells that expressed human p2x7 receptors, a 804598 inhibited bzatp stimulated yo-pro uptake and release of il-1β. in 1321n1 cells expressed recombinant rat p2x7 receptor, a 804598 showed high affinity with kd = 2.4 nm [1]. a 804598 inhibited bz-atp stimulated calcium influx with ic50 value of 28.71 nm in a concentration-dependent way. a-804598 was a potent p2x7 receptor antagonist with ki value of 7.51 nm [2].in adult male rats, footshock increased the mrna levels of cd14 and il-1β in the paraventricular nucleus. while a-804598 (25 mg/kg) partially inhibited these effects [3].
Lager
Store at -20°C
Einzelnachweise
[1]. donnelly-roberts dl, namovic mt, surber b, et al. [3h]a-804598 ([3h]2-cyano-1-[(1s)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for p2x7 receptors. neuropharmacology, 2009, 56(1): 223-229.
[2]. able sl, fish rl, bye h, et al. receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant p2x7 antagonists in the rat. br j pharmacol. 2011, 162(2): 405-414.
[3]. catanzaro jm1, hueston cm, deak mm, et al. the impact of the p2x7 receptor antagonist a-804598 on neuroimmune and behavioral consequences of stress. behav pharmacol, 2014, 25(5-6): 582-598.

A 804598 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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