ML348

製品コードS6564 バッチS656404

印刷

化学情報

Chemical Structure Synonyms GNF-Pf-1127 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C18H17ClF3N3O3
分子量 415.79 CAS No. 899713-86-1
Solubility (25°C)* 体外 DMSO 30 mg/mL (72.15 mM)
Ethanol 21 mg/mL (50.5 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ML348 (GNF-Pf-1127) is a potent and selective APT1 (Acyl protein thioesterase 1)/lysophospholipase 1 (LYPLA1) inhibitor with Ki values of 280 nM and >10 μM for APT1 and APT2, respectively.
in vitro

ML348 increases brain palmitoylation and inhibits the palmitate-removing enzyme acyl-protein thioesterase 1 (APT1), restores axonal transport, synapse homeostasis, and survival signaling to wild-type levels without toxicity, also increases BDNF trafficking in human HD induced pluripotent stem cell-derived cortical neurons.[2]
in vivo

In HD knock-in mice, ML348 efficiently crosses the blood-brain barrier to restore palmitoylation levels and reverse neuropathology, locomotor deficits, and anxio-depressive behaviors.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 STHdh cells, human HD patient iPSC-derived cortical neurons, CAG140 neurons
濃度 10, 1 μM
反応時間 1, 4h
実験の流れ

ML348, palmostatin B, and ML349 are diluted in 100% dimethyl sulfoxide (DMSO) for primary concentration. For STHdh cells and immunofluorescence of neurons plated on coverslips, we administered acute treatment with 10 μM for 1 hour before and during the acquisition time. For the fractionation experiments, we plated cortical neurons on 10-cm dishes and we treated cells for 4 hours with 1 μM ML348 before lysis. For neurons within microchambers, 1 μM ML348 is administered within each compartment of the microfluidic device beginning on days in vitro (DIV)2 and continuing daily until DIV12, while for BDNF pHluorin analysis, compartments are treated for 4 hours with 1 μM ML348 before acquisition.
動物実験 動物モデル HdhCAG140/+ knock-in mice (CAG140), Thy1:p50-GFP HdhCAG111/+ mice
投薬量 2 mg/kg
投与方法 i.p.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。