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Verubecestat is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor. Verubecestat was found to reduce amyloid in plasma, cerebral spinal fluid, and brains in several animal models. However, development of verubecestat as a treatment was halted when it was shown to have no impact on slowing the progression of Alzheimer’s disease.
| Cas No. | 1286770-55-5 |
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| Purity | ≥98% |
| Formula | C17H17F2N5O3S |
| Formula Wt. | 409.41 |
| Chemical Name | N-(3-(3-amino-5,6-dihydro-2,5-dimethyl-1,1-dioxido-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoro-2-pyridinecarboxamide |
| IUPAC Name | N-[3-[(5R)-3-amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide |
| Synonym | MK-8931, MK8931 |
| Solubility | DMSO:81 mg/mL (197.84 mM); Ethanol:41 mg/mL (100.14 mM); Water:Insoluble |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Villarreal S, Zhao F, Hyde LA, et al. Chronic verubecestat treatment suppresses amyloid accumulation in advanced aged Tg2576-AbPPswe mice without inducing microhemorrhage. J Alzheimers Dis. 2017;59(4):1393-1413. PMID: 28800329.
Kennedy ME, Stamford AW, Chen X, et al. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS beta-amyloid in animal models and in Alzheimer’s disease patients. Sci Transl Med. 2016 Nov 2;8(363):363ra150. PMID: 27807285.
Oblak A, Cope Z, Quinney S, et al. Prophylactic evaluation of verubecestat on disease-and symptom-modifying effects in 5XFAD mice. Alzheimers Dement (N Y). 2022 Jul 14;8(1):e12317. PMID: 35846156.
Watamura N, Sato K, Shiihashi G, et al. An isogenic panel of App knock-in mouse models: profiling beta-secretase inhibition and endosomal abnormalities. Sci Adv. 2022 Jun 10;8(23):eabm6155. PMID: 35675411.