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Semagacestat

Cat. No. M2277

All AbMole products are for research use only, cannot be used for human consumption.

Semagacestat Structure
Synonym:

LY450139

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 33  USD33 In stock
5mg USD 60  USD60 In stock
10mg USD 110  USD110 In stock
50mg USD 390  USD390 In stock
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Quality Control & Documentation
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.
Chemical Information
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
References

[1] Guanghui Yang, et al. Structural basis of γ-secretase inhibition and modulation by small molecule drugs

[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

[4] Harrit Schellekens, et al. Semagacestat, a γ-secretase inhibitor, activates the growth hormone secretagogue (GHS-R1a) receptor

[5] David B Henley, et al. Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease

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Keywords: Semagacestat, LY450139 supplier, Gamma-secretase/Beta-secretase, inhibitors, activators

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