Description
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
Product information
CAS Number: 1311174-68-1
Molecular Weight: 491.58
Formula: C27H33N5O4
Chemical Name: tert-butyl 4-({4-[2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamido]phenyl}methyl)piperazine-1-carboxylate
Smiles: CN1N=C(CC(=O)NC2=CC=C(CN3CCN(CC3)C(=O)OC(C)(C)C)C=C2)C2C=CC=CC=2C1=O
InChiKey: GSXXTLWPQMHHDJ-UHFFFAOYSA-N
InChi: InChI=1S/C27H33N5O4/c1-27(2,3)36-26(35)32-15-13-31(14-16-32)18-19-9-11-20(12-10-19)28-24(33)17-23-21-7-5-6-8-22(21)25(34)30(4)29-23/h5-12H,13-18H2,1-4H3,(H,28,33)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 75 mg/mL (152.57 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells, with an IC50 of 116 nM in FRET.
In Vivo:
PH-002 is also shown to increase COX1 levels in primary neurons from NSE-apoE4 transgenic mouse cortex and hippocampus. After 4 days of treatment with PH-002 (200 nM), COX1 levels are increased by ~60%. PH-002 (100 nM) increases dendritic spine development in primary neurons from NSE-apoE4 transgenic mice to levels comparable with those in NSE-apoE3 primary neurons (apoE3-expressing primary neurons treated with PH-002 gave results identical to untreated primary neurons).
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