ChemicalBook > CAS DataBase List > MK-8931
MK-8931
MK-8931
- CAS No.1286770-55-5
- Chemical Name:MK-8931
- CBNumber:CB22756736
- Molecular Formula:C17H17F2N5O3S
- Formula Weight:409.41
- MOL File:1286770-55-5.mol
MK-8931 Property
- 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
- FDA UNII J1I0P6WT7T
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
MK-8931 Chemical Properties,Usage,Production
- 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
- IC 50 BACE1; BACE2
- 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-8931 Preparation Products And Raw materials
Raw materials
Preparation Products
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1286770-55-5, MK-8931Related Search:
- 抑制剂
- 合成有机化合物配体
- 维罗司他,10 MM DMSO 溶液
- MK-8931,BETA-SECTETASE抑制剂
- 维罗司他(MK-8931) (BACE1/2抑制剂)
- 维罗司他(MK-8931)
- (R)-N-(3-(3-氨基-2,5-二甲基-1,1-二氧代-5,6-二氢-2H-1,2,4-噻二嗪-5-基)-4-氟苯基)-5-氟吡啶-2-甲酰胺
- N-[3-[(5R)-3-氨基-5,6-二氢-2,5-二甲基-1,1-二氧化物2H-]1,2,4-噻二嗪--5-基]-4-氟苯基]-5-氟-2-吡啶甲酰胺
- 维罗司他
- 1286770-55-5
- Verubecestat, 10 mM in DMSO
- MK-8931, Beta-sectetase inhibitor
- orally,Beta-secretase,β-Secretase,inhibit,Aβ40,BACE1,MK8931,Alzheimer's,BACE,Inhibitor,MK 8931,Disease,BACE2,Verubecestat
- 2-Pyridinecarboxamide, N-[3-[(5R)-3-amino-5,6-dihydro-2,5-dimethyl-1,1-dioxido-2H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoro-
- CS-2556
- MK8931;MK 8931;MK-8931
- MK-8931 Trifluoroacetat
- Verubecestat free base
- SCH-900931
- SCH900931
- SCH 900931
- MK-8931-009
- MK-8931; MK 8931; MK8931; MK-8931-009; SCH 900931; SCH-900931; SCH900931; VERUBECESTAT FREE BASE,
- MK-8931(Verubecestat)
- (R)-N-(3-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoropicolinamide
- Verubecestat (MK-8931)
- N-[3-[(5R)-3-Amino-5,6-dihydro-2,5-dimethyl-1,1-dioxido-2H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide
- Verubecestat