2071636-15-0

Name	Lp-PLA2-IN-2
CAS	2071636-15-0
Molecular Formula	C19H23FN2O4S
MDL Number	MFCD34469888
Molecular Weight	394.46
MOL File	2071636-15-0.mol

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]-

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Chemical Properties

Boiling point	637.6±55.0 °C(Predicted)
density	1.34±0.1 g/cm3(Predicted)
pka	-0.95±0.40(Predicted)

Hazard Information

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 t_1/2 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 t_1/2 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

Supplier

Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 15801484223;

Websitehttp://www.jm-bio.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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