5.32978
PLD2 Inhibitor, ML395
Synonym(s):
PLD2 Inhibitor, ML395, Phosppolipase D2 inhibitor, VU0468809, ML-395
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About This Item
Empirical Formula (Hill Notation):
C26H29N5O2
CAS Number:
Molecular Weight:
443.54
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
solid
potency
360 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
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).
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.
Biochem/physiol Actions
Primary Target
PLD2
PLD2
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).
Other Notes
O′Reilly, M.C., et al. 2014. ChemMedChem9, 2633.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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