| Identification | Back Directory | [Name]
Lp-PLA2-IN-2 | [CAS]
2071636-15-0 | [Synonyms]
Lp-PLA2-IN-2
LpPLA2IN2,Lp-PLA-2-IN-2,Lp PLA2 IN 2
Benzonitrile, 2-fluoro-5-[2-[(4S)-2-oxo-4-(tetrahydro-4-methyl-1,1-dioxido-2H-thiopyran-4-yl)-1-pyrrolidinyl]ethoxy]- | [Molecular Formula]
C19H23FN2O4S | [MDL Number]
MFCD34469888 | [MOL File]
2071636-15-0.mol | [Molecular Weight]
394.46 |
| Hazard Information | Back Directory | [Uses]
Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2[1]. | [in vivo]
Lp-PLA2-IN-2 (1 mg/kg; i.v.) treament in rats shows that the Cl, Vss and t1/2 values are 67 mL/min/kg, 1.2 L/kg, and 0.34 hours, respectively[1]. | Animal Model: | Male Han Wistar rats (250-300 g)[1] | | Dosage: | 1 mg/kg | | Administration: | i.v. (Pharmacokinetic Analysis) | | Result: | The Cl, Vss and t1/2 values were 67 mL/min/kg, 1.2 L/kg, and 0.34 hours, respectively. |
| [IC 50]
Lp-PLA2: 120 nM (IC50) | [References]
[1] Woolford AJ, et al. Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2). J Med Chem. 2016 Dec 8;59(23):10738-10749. DOI:10.1021/acs.jmedchem.6b01427 |
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