DARAPLADIB

Bezeichnung:DARAPLADIB

CAS-Nr356057-34-6

Englisch Name:DARAPLADIB

CBNumberCB21011731

SummenformelC36H38F4N4O2S

Molgewicht666.77

MOL-Datei356057-34-6.mol

DARAPLADIB physikalisch-chemischer Eigenschaften

Siedepunkt	741.0±70.0 °C(Predicted)
Dichte	1.25
storage temp.	Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH
Aggregatzustand	solid
pka	9.03±0.10(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

DARAPLADIB Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Treatment of atherosclerosis.
Verwenden
Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor.
Biologische Aktivität
plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. lipoprotein-associated phospholipase a2 (lp-pla2) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. darapladib is a selective inhibitor of lp-pla2.
in vitro
darapladib potently inhibited lp-pla2 with an ic50 of 270 pm. a lack of selectivity against other secretory pla2s postulated to play a role in atherogenesis had been demonstrated. the percentage inhibition achieved when 1 μm darapladib was evaluated against human secretory pla2s iia, v and x, was 0, 0 and 8.7%, respectively [1].
in vivo
inhibition of lp-pla2 by darapladib led to attenuation of inflammation in vivo and decreased plaque formation in apoe-deficient mice, suggesting an anti-atherogenic role during the progression of atherosclerosis [2].
target
Lp-PLA2
Lager
Store at -20°C
Einzelnachweise
[1] bui qt, wilensky rl. darapladib. expert opin investig drugs. 2010;19(1):161-8.
[2] wang wy, zhang j, wu wy, li j, ma yl, chen wh, yan h, wang k, xu ww, shen jh, wang yp. inhibition of lipoprotein-associated phospholipase a2 ameliorates inflammation and decreases atherosclerotic plaque formation in apoe-deficient mice. plos one. 2011;6(8):e23425.
[3] mohler er 3rd, ballantyne cm, davidson mh, hanefeld m, ruilope lm, johnson jl, zalewski a; darapladib investigators. the effect of darapladib on plasma lipoprotein-associated phospholipase a2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. j am coll cardiol. 2008;51(17):1632-41.

DARAPLADIB Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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