[CAS NO. 1194044-20-6] LY2811376
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PRODUCTS SPECIFICATIONS [1194044-20-6]
Store
Catalog
SLK-S1528
Brand
Selleck
CAS
1194044-20-6
DESCRIPTION [1194044-20-6]
Overview
| MDL | MFCD18074525 |
|---|---|
| Molecular Weight | 320.36 |
| Molecular Formula | C15H14F2N4S |
| SMILES | NC1=N[C@](C)(C2=CC(C3=CN=CN=C3)=C(F)C=C2F)CCS1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1215 mL | 15.6074 mL | 31.2149 mL |
| 5 mM | 0.6243 mL | 3.1215 mL | 6.2430 mL |
| 10 mM | 0.3121 mL | 1.5607 mL | 3.1215 mL |
| 50 mM | 0.0624 mL | 0.3121 mL | 0.6243 mL |
Description
LY2811376 is the first orally available non-peptidic inhibitor with of 239 nM-249 nM, that act to decrease Aβ secretion with of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1.
Features
Approximately 10-fold selectivity toward BACE1 over BACE2.
In vitro
LY2811376 demonstrates concentration-dependent inhibition of hBACE1 with an IC50 of 239 and 249 nM against a small synthetic peptide or a larger chimeric protein substrate, respectively. LY2811376 treatment yields a concentration-dependent decrease in Aβ secretion in APP-overexpressing HEK293 cells. LY2811376 inhibits Aβ secretion with EC50 of ~100 nM in primary neuronal cultures of PDAPP transgenic mouse.
In vivo
Administration of LY2811376 (10, 30, and 100 mg/kg doses) results in dose-dependent, significant reductions in Aβ, as well as sAPPβ and C99, the proximal cleavage products of APP proteolysis by BACE1 in APP mouse model of Aβ pathology. After treatment with LY2811376 (5 mg/kg), reductions in Aβ are observed in plasma, with a maximal 85% reduction observed from 4 to 12 h after dosing in beagle dogs.
References
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