SB-435495 (ditartrate)

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].

Product Specifications

CAS Number

[304694-43-7]

UNSPSC

12352005

Target

Phospholipase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/sb-435495-ditartrate.html

Solubility

10 mM in DMSO

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

Molecular Formula

C46H52F4N6O14S

Molecular Weight

1021.00

References & Citations

[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.|[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.|[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.