851600-86-7
851600-86-7 structure
- Name: ELN 318463
- Chemical Name: ELN 318463
- CAS Number: 851600-86-7
- Molecular Formula: C19H20BrClN2O3S
- Molecular Weight: 471.80
- Catalog: Research Areas Neurological Disease
- Create Date: 2020-06-01 23:27:20
- Modify Date: 2024-01-09 18:10:00
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ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN 318463 is 51-fold more selective for PS1[1][2].
| Name | ELN 318463 |
|---|
| Description | ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN 318463 is 51-fold more selective for PS1[1][2]. |
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| Related Catalog | |
| Target |
EC50: 12 nM (PS1 γ-secretase), 656 nM (PS2 γ-secretase)[1] |
| In Vitro | ELN 318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate[2]. |
| In Vivo | ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice[2]. Animal Model: Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)[2] Dosage: 30 mg/kg or 100 mg/kg Administration: Orally Result: Brain levels at 30 mg/kg were 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains. |
| References |
| Molecular Formula | C19H20BrClN2O3S |
|---|---|
| Molecular Weight | 471.80 |