| Identification | Back Directory | [Name]
1(4H)-Pyrimidineacetamide, N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-, (2R,3R)-2,3-dihydroxybutanedioate (1:2) | [CAS]
304694-43-7 | [Synonyms]
1(4H)-Pyrimidineacetamide, N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-, (2R,3R)-2,3-dihydroxybutanedioate (1:2) | [Molecular Formula]
C42H46F4N6O8S | [MOL File]
304694-43-7.mol | [Molecular Weight]
870.92 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | Animal Model: | WHHL rabbit[1] | | Dosage: | 10 mg/kg | | Administration: | Oral, once | | Result: | Inhibited plasma Lp-PLA2 in the WHHL rabbit. |
| [IC 50]
Lp-PLA2: 0.06 nM (IC50) | [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. DOI:10.1016/s0960-894x(02)00473-0
[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. DOI:10.3892/etm.2017.4142
[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. DOI:10.1073/pnas.1514213113 |
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