5.32978

PLD2 Inhibitor, ML395

• 동의어(들): PLD2 Inhibitor, ML395, Phosppolipase D2 inhibitor, VU0468809, ML-395
• 실험식(Hill 표기법): C₂₆H₂₉N₅O₂
• CAS Number: 1638957-17-1
• Molecular Weight: 443.54
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: solid
• 효능: 360 nM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

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).

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.

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.

생화학적/생리학적 작용

Primary Target
PLD2

Reversible: yes

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable