Lp-PLA2-IN-2

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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.

For research use only. We do not sell to patients.

Lp-PLA2-IN-2 Chemical Structure

CAS No. : 2071636-15-0

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Description

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].

IC₅₀ & Target^[1]

Lp-PLA2

120 nM (IC₅₀)

In Vitro

Lp-PLA2-IN-2 inhibits Human Lp-PLA2 with an IC₅₀ of 62 nM in PED6 assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

394.46

Formula

C₁₉H₂₃FN₂O₄S

CAS No.

2071636-15-0

SMILES

N#CC1=CC(OCCN2C(C[C@@H](C(CC3)(C)CCS3(=O)=O)C2)=O)=CC=C1F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

Lp-PLA2-IN-2 Related Classifications

Inflammation/Immunology

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lp-PLA2-IN-22071636-15-0PhospholipaseLp-PLA2inflammationdiseaseslactamphospholipaseselectiveInhibitorinhibitorinhibit

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