ML348

製品コードS6564 バッチS656401

印刷

化学情報

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

83 mg/mL (199.62 mM)

Ethanol

10 mg/mL (24.05 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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 this compound before lysis. For neurons within microchambers, 1 μM this chemical 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 this compound 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.

参考

https://www.ncbi.nlm.nih.gov/pubmed/?term=28065656
https://pubmed.ncbi.nlm.nih.gov/33789888/

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。