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Semagacestat

Cat. No. M2277
Semagacestat Structure
Synonym:

LY450139

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 29.7  USD33 In stock
5mg USD 54  USD60 In stock
10mg USD 99  USD110 In stock
50mg USD 351  USD390 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.

Product Citations
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
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.
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 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.

Chemical Information
Molecular Weight 361.44
Formula C19H27N3O4
CAS Number 425386-60-3
Purity 97.69%
Solubility DMSO 62 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




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

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