PLD2 Inhibitor; ML395 1PC X 10MG

Biochem/physiol Actions

Reversible: yes

Primary TargetPLD2

General description

ML395 is a cell permeable, highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC₅₀ = 360 nM) that exhibits >80-fold selectivity over PLD1.

A cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC₅₀ = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC₅₀ = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski′s rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC₅₀ = 3.9 µM, CYP2D6 IC₅₀ =16.4 µM, CYP1A2 IC₅₀>30 µM, and CYP2C9 IC₅₀>30 µM).Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC₅₀ = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC₅₀ = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski′s rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC₅₀ = 3.9 µM, CYP2D6 IC₅₀ =16.4 µM, CYP1A2 IC₅₀>30 µM, and CYP2C9 IC₅₀>30 µM).

Legal Information

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

Other Notes

O′Reilly, M.C., et al. 2014. ChemMedChem9, 2633.

Packaging

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)