2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Amyloid-β
  4. EVP-0015962

EVP-0015962 is an orally active, blood-brain barrier-permeable γ-secretase inhibitor with an IC50 of 3.9 μM. EVP-0015962 alters γ-secretase-mediated cleavage of amyloid precursor protein, reduces Aβ42 production and increases Aβ38 production. EVP-0015962 reduces Aβ aggregates, amyloid plaques and inflammatory markers in the brains of mice, and improves their cognitive impairment. EVP-0015962 can be used for the research of Alzheimer's disease.

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EVP-0015962

EVP-0015962 Chemical Structure

CAS No. : 1447811-26-8

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Description

EVP-0015962 is an orally active, blood-brain barrier-permeable γ-secretase inhibitor with an IC50 of 3.9 μM. EVP-0015962 alters γ-secretase-mediated cleavage of amyloid precursor protein, reduces Aβ42 production and increases Aβ38 production. EVP-0015962 reduces Aβ aggregates, amyloid plaques and inflammatory markers in the brains of mice, and improves their cognitive impairment. EVP-0015962 can be used for the research of Alzheimer's disease[1].

In Vitro

EVP-0015962 (0.003-10 μM; 16-18 h) acts as a γ-secretase modulator in H4-APP751 cells, potently decreasing Aβ42 (IC50 = 67 nM) and increasing Aβ38 without altering total Aβ levels at non-cytotoxic concentrations[1].
EVP-0015962 (0.01-30 μM; 24 h) modulates γ-secretase in rat primary neocortical cultures, decreasing Aβ42 (IC50 = 427 nM) and increasing Aβ38 without reducing Aβ1-ₓ levels or inducing cytotoxicity at active concentrations[1].
EVP-0015962 (0.001-100 μM; 3 h) modulates γ-secretase in a cell-free reconstituted system, selectively lowering Aβ42 (IC50 = 3.9 μM) without inhibiting AICD production or altering Aβ40 levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EVP-0015962 Related Antibodies
In Vivo

EVP-0015962 (10-30 mg/kg; p.o.; single dose) significantly reduces brain Aβ42 levels by 39% in 21-week-old male Tg2576 mice[1].
EVP-0015962 (20-60 mg/kg/day; p.o.; continuous via food formulation; 50 weeks) is well-tolerated in male Tg2576 mice, reduces brain Aβ42 levels by 53-89%, aggregated Aβ by 73% at the high dose, amyloid plaque burden, and reactive gliosis, with a dose-dependent trend in efficacy[1].
EVP-0015962 (20-60 mg/kg/day; p.o.; continuous via food formulation; 11 weeks) reverses the contextual fear conditioning cognitive deficit in 30-33-week-old male Tg2576 mice[1].
EVP-0015962 (30 mg/kg; p.o.; single dose) does not reverse the contextual fear conditioning cognitive deficit in 30-week-old male Tg2576 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tg2576 (B6;SJL-Tg(APPSWE)2576Kha) (male, 21 weeks old, 24-35 g)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Reduced brain Aβ42 levels by 22% relative to vehicle controls (not statistically significant).
Reduced brain Aβ42 levels by 39% relative to vehicle controls.
Left AβTotal levels unchanged with both doses.
Animal Model: Tg2576 (B6;SJL-Tg(APPSWE)2576Kha) (male, 17-26 weeks old at study start)[1]
Dosage: 20 mg/kg/day; 60 mg/kg/day
Administration: p.o.; continuous via food formulation; 50 weeks
Result: Achieved brain concentrations of 2.5 μM (20 mg/kg/day group) and 8.3 μM.
Reduced TBS-soluble Aβ42 by 53% in the 20 mg/kg/day group and 89% in the 60 mg/kg/day group relative to controls.
Reduced formic acid-extractable Aβ42 by 53% in the 20 mg/kg/day group and 86% in the 60 mg/kg group relative to controls.
Increased TBS-soluble Aβ38 by 78% in the 60 mg/kg/day group relative to controls; the 20 mg/kg/day group showed no significant increase.
Reduced formic acid-extractable AβTotal by 49% in the 20 mg/kg/day group and 64% in the 60 mg/kg/day group relative to controls.
Animal Model: Tg2576 (B6;SJL-Tg(APPSWE)2576Kha) (male, 19-22 weeks old at study start, tested at 30-33 weeks old)[1]
Dosage: 20 mg/kg/day; 60 mg/kg/day
Administration: p.o.; continuous via food formulation; 11 weeks
Result: Reversed the cognitive deficit (reduced percent freezing) in Tg2576 mice completely, with percent freezing levels in both treatment groups not significantly different from wild-type controls and significantly higher than control diet Tg2576 mice.
Animal Model: Tg2576 (B6;SJL-Tg(APPSWE)2576Kha) (male, 30 weeks old)[1]
Dosage: 30 mg/kg
Administration: p.o.; single dose
Result: Did not reverse the genotype-associated cognitive deficit (reduced percent freezing) in Tg2576 mice relative to wild-type mice; percent freezing levels in EVP-0015962-treated Tg2576 mice remained significantly lower than those in EVP-0015962-treated wild-type mice.
Molecular Weight

480.83

Formula

C22H19ClF6O3
CAS No.
SMILES

O=C([C@@H](C1=CC(C2=CC=C(C=C2)C(F)(F)F)=C(C(Cl)=C1)OCC(F)(F)F)CC3CCC3)O
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EVP-00159621447811-26-8EVP0015962EVP 0015962γ-secretaseAmyloid-βGamma secretaseβ-amyloid peptideAβAbetaAβ38alzheimer’s diseaseH4-APP751 cellsHEK293 cellsγ-secretase complexamyloid precursor proteinamyloid plaquesTg2576 mouserat primary neocortical culturesAβ42Inhibitorinhibitorinhibit

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