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Semagacestat

Cat. No. M2277
Semagacestat Structure
Synonym:

LY450139

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 480 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 361.44
Formula C19H27N3O4
CAS Number 425386-60-3
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Science Advance (2017). semagacesta, Figure 6. (AbMole Bioscience)
Method
Cell Lines
Concentrations 10mg/kg
Incubation Time
Results We showed that semagacestat was able to rescue levels of both NaV1.1 andNaV1.6, while LY2811376 only rescued those of NaV1.6 (one-way ANOVA for NaV1.1: F3,23 = 6.52, P = 0.0024; one-way ANOVA for NaV1.6: F3,23 = 5.911, P = 0.0038; Fig. 6). Therefore, beneficial effects of b- and g-secretase inhibitor treatments on the spatial object location task might be mediated, in part, by a rescue of the NaV levels, thereby restoring “normal” PV interneuron function
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Source Science Advance (2017). semagacesta, Figure 5. (AbMole Bioscience)
Method
Cell Lines
Concentrations 10mg/kg
Incubation Time
Results In addition, we also confirmed that hippocampal b-CTF contents were decreased following the LY2811376 treatment but increased after the semagacestat treatment (one-sample t test against TgCRND8-vehicle: TgCRND8-LY2811376: t4 = 14.42, P = 0.0001; TgCRND8-semagacestat: t8 = 14.30, P < 0.0001). Given the distinct effect of LY2811376 and semagacestat treatments on both APP metabolite levels and cognitive performances, it is likely that different APP metabolites are responsible for the deficits of TgCRND8 mice in the spatial object location task and in the objectplace association task.
Rating
Product Citations
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Semagacestat, LY450139 supplier, Gamma-secretase, inhibitors

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