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Synonyms | GNF-Pf-1127 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C18H17ClF3N3O3 |
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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 | |||
* <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. |
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. |
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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] |
細胞アッセイ | 細胞株 | STHdh cells, human HD patient iPSC-derived cortical neurons, CAG140 neurons |
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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. |
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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. |
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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。
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