ApoE4 Modulator, PH002-Calbiochem

C₂₇H₃₃N₅O₄

491.58

MFCD22666400

A phthalazinone derived compound that directly binds to the 22-kDa amino-terminal region of apolipoprotein E4 (ApoE4) and blocks its intramolecular domain interactions in neuronal cells (IC₅₀ = 116 nM) thereby reversing the detrimental effects of ApoE4. Established to be more potent than GIND25. Restores mitochondrial functions and elevates the levels of complex IV subunit 1. Shown to increase in COX1 levels in primary neurons from NSE-ApoE4 transgenic mouse cortex and hippocampus. Shown to rescue impairments of mitochondrial motility in primary neurons from NSE-ApoE4 transgenic mice (~ 200 nM). Also restores endoplasmic reticulum and Golgi apparatus transit of ApoE4 in cultured neurons and brings it to levels normally found in ApoE3 and ApoE4-R61T.

Cell permeable: yes
Primary Target
APOE4
Reversible: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Chen, H., et al. 2011. J. Biol. Chem.287, 5253.
Brodbeck, J., et al. 2011. J. Bio. Chem.286, 17217.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥99% (HPLC)

powder

116 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 100 mg/mL, clear, colorless

wet ice

2-8℃

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3