Semagacestat (LY450139) is a γ-secretase blocker with an IC50 of 15 nM. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM. Semagacestat blocks the enzyme γ-secretase, which (along with β-secretase) is responsible for APP proteolysis.
Cytotechnology. 2019 Oct;71(5):881-891.
TGF-β1 signaling activates hepatic stellate cells through Notch pathway.
Semagacestat purchased from AbMole
Sci Adv. 2017 Feb 24;3(2):e1601068.
Differential contribution of APP metabolites to early cognitive deficits in a TgCRND8 mouse model of Alzheimer’s disease
Semagacestat purchased from AbMole
Molecular Weight | 361.44 |
Formula | C19H27N3O4 |
CAS Number | 425386-60-3 |
Solubility (25°C) | DMSO 62 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Shinji Tagami, et al. Semagacestat Is a Pseudo-Inhibitor of γ-Secretase
[3] Rachelle S Doody, et al. A phase 3 trial of semagacestat for treatment of Alzheimer's disease
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