Basic information Safety Supplier Related

MK-8931

Basic information Safety Supplier Related

MK-8931 Basic information

Product Name:
MK-8931
Synonyms:
  • MK-8931; MK 8931; MK8931; MK-8931-009; SCH 900931; SCH-900931; SCH900931; VERUBECESTAT FREE BASE,
  • MK-8931-009
  • SCH 900931
  • SCH900931
  • SCH-900931
  • Verubecestat free base
  • MK-8931 Trifluoroacetat
  • Verubecestat
CAS:
1286770-55-5
MF:
C17H17F2N5O3S
MW:
409.41
Mol File:
1286770-55-5.mol
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MK-8931 Chemical Properties

Melting point:
160-162oC
Density 
1.52±0.1 g/cm3(Predicted)
storage temp. 
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
9.92±0.70(Predicted)
form 
Solid
color 
White
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MK-8931 Usage And Synthesis

Uses

Verubecestat is used in a β-site amyloid precursor protein cleaving enzyme I inhibitor of treatment of alzheimer’s disease.

Biological Activity

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

storage

Store at -20°C

References

[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-8931Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 17702719238
Email
sales@sun-shinechem.com
UHN Shanghai Research & Development Co., Ltd.
Tel
021-58958002 18930822973
Email
SALES@UHNSHANGHAI.COM
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
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MK-8931(1286770-55-5)Related Product Information