SB-435495 ditartrate

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SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA₂ inhibitor with an IC₅₀ of 0.06 nM.

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SB-435495 ditartrate Chemical Structure

CAS No. : 304694-43-7

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Phospholipase A PLD

Biological Activity
Purity & Documentation
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Description

SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA₂ inhibitor with an IC₅₀ of 0.06 nM^[1]^[3].

IC₅₀ & Target^[1]

Lp-PLA2

0.06 nM (IC₅₀)

In Vitro

SB-435495 ditartrate inhibits CYP450 3A4 with an IC₅₀ of 10 μM and the black membrane permeability is 0.017 cm/h^[1].
SB-435495 (5 μM; 24 h) ditartrate significantly inhibits the expression of Lp-PLA₂ protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs^[2].
SB-435495 (5 μM; 24-72 h) ditartrate significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs^[2].

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

Western Blot Analysis^[2]

Cell Line:	oxLDL-exposed human umbilical vein endothelial cells
Concentration:	5 μM
Incubation Time:	24 h
Result:	The expression of Lp-PLA₂ protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172).

Cell Viability Assay^[2]

Cell Line:	oxLDL-exposed human umbilical vein endothelial cells
Concentration:	5 μM
Incubation Time:	24, 48 and 72 h
Result:	Significantly increased cell viability.

In Vivo

SB-435495 (10 mg/kg; p.o.; once) ditartrate inhibits plasma Lp-PLA₂ in the WHHL rabbit^[1].
SB-435495 (10 mg/kg; i.p.; daily for 28 days) ditartrate effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin (HY-13753)-diabetic Brown Norway rats^[3].

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

Animal Model:	WHHL rabbit^[1]
Dosage:	10 mg/kg
Administration:	Oral, once
Result:	Inhibited plasma Lp-PLA₂ in the WHHL rabbit.

Molecular Weight

1021.00

Formula

C₄₆H₅₂F₄N₆O₁₄S

CAS No.

304694-43-7

SMILES

O=C(N(CCN(CC)CC)CC1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)CN(C(SCC3=CC=C(F)C=C3)=N4)C=C(CC5=CN(C)N=C5)C4=O.OC([C@H](O)[C@@H](O)C(O)=O)=O.OC([C@H](O)[C@@H](O)C(O)=O)=O

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]. Blackie JA, et al. The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. [Content Brief]

[2]. Yang L, et al. AMP-activated protein kinase mediates the effects of lipoprotein-associated phospholipase A2 on endothelial dysfunction in atherosclerosis. Exp Ther Med. 2017 Apr;13(4):1622-1629. [Content Brief]

[3]. Canning P, et al. Lipoprotein-associated phospholipase A2 (Lp-PLA2) as a therapeutic target to prevent retinal vasopermeability during diabetes. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7213-8. [Content Brief]