PLD2 Inhibitor, ML395 – Calbiochem

Descrição detalhada : 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).
Sinónimos : PLD2 Inhibitor, ML395 - Calbiochem; Phosppolipase D2 inhibitor, VU0468809, ML-395
Fórmula molecula r: C26H29N5O2
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X1EA