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ML348 Phospholipase (e.g. PLA) inhibitor

Cat.No.S6564

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.
ML348 Phospholipase (e.g. PLA) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 415.79

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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.62 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 415.79 Formula

C18H17ClF3N3O3

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 899713-86-1 -- Storage of Stock Solutions

Synonyms GNF-Pf-1127 Smiles C1CN(CCN1CC(=O)NC2=C(C=CC(=C2)C(F)(F)F)Cl)C(=O)C3=CC=CO3

Mechanism of Action

Targets/IC50/Ki
APT1
280 nM(Ki)
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.

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.

References

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