178477

ApoE4 Modulator, PH002

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 thereby reversing the detrimental effects of ApoE4.

• 別名: ApoE4 Modulator, PH002, 4-{4-[2-(3-methyl-4-oxo-3,4-dihydro-phthalazin-1-yl)-acetylamido]-benzyl}-piperazine-1-carboxylic acid tert-butyl ester, ApoE4 Structure Corrector, PH-002, Apolipoprotein E4 structure corrector
• 実験式（ヒル表記法）: C₂₇H₃₃N₅O₄
• CAS番号: 1311174-68-1
• 分子量: 491.58
• MDL番号: MFCD22666400
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥99% (HPLC)
• フォーム: powder
• 有効性: 116 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL, clear, colorless
• 輸送温度: wet ice
• 保管温度: 2-8°C
• SMILES記法: N4(CCN(CC4)C(=O)OC(C)(C)C)Cc1ccc(cc1)NC(=O)C=C2NN(C(=O)c3c2cccc3)C
• InChI Key: HABKFQXKIOOEIG-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
APOE4

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable