MK-8931 Struktur

MK-8931

Bezeichnung:MK-8931

CAS-Nr1286770-55-5

Englisch Name:MK-8931

CBNumberCB22756736

SummenformelC17H17F2N5O3S

Molgewicht409.41

MOL-Datei1286770-55-5.mol

MK-8931 physikalisch-chemischer Eigenschaften

Schmelzpunkt	160-162oC
Dichte	1.52±0.1 g/cm3(Predicted)
storage temp.	Keep in dark place,Sealed in dry,Store in freezer, under -20°C
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
pka	9.92±0.70(Predicted)
Aggregatzustand	Solid
Farbe	White

Gefahreninformationscode (GHS)

MK-8931 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Verubecestat is used in a β-site amyloid precursor protein cleaving enzyme I inhibitor of treatment of alzheimer’s disease.
Biologische Aktivität
ki: 2.2 and 3.4 nm for human and mouse bace1, respectivelyverubecestat (mk-8931) is a bace1 inhibitor.β-amyloid (aβ) peptides are regarded to be involved in the etiology of ad. bace1 is required for the aβ production, and bace1 inhibition is therefore an promising target for the ad treatment.
in vitro
verubecestat has been identified as a potent inhibitor of both human and mouse bace1 and verubecestat could also inhibit the production of ab40, ab42, and sappb in human cells with similar potency. verubecestat was also found to be a potent inhibitor of purified human bace2. moreover, verubecestat was essentially inactive with over 45,000-fold selectivity in the purified human aspartyl proteases cathepsin d, cathepsin e, and pepsin and had a very weak inhibitor of purified human renin with 15,000-fold selectivity. in addition, verubecestat was also found to have minimal or no activity against various tested receptors, ion channels, transporters, as well as enzymes [1].
in vivo
verubecestat could reduce plasma, cerebrospinal fluid, and brain concentrations of aβ40, aβ42, and sappβ after acute and chronic administration to both rats and monkeys. moreover, the chronic treatment of rats and monkeys with verubecestat at exposures >40-fold higher than those tested in
Lager
Store at -20°C
Einzelnachweise
[1] kennedy me et al. the bace1 inhibitor verubecestat (mk-8931) reduces cns β-amyloid in animal models and in alzheimer's disease patients. sci transl med.2016 nov 2;8(363):363ra150.

MK-8931 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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