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Home - Products - Metabolic Enzyme/Protease - Phospholipase - SB-435495

SB-435495

CAS No. 304694-39-1

SB-435495( SB435495 )

Catalog No. M13964 CAS No. 304694-39-1

SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 110 In Stock
5MG 70 In Stock
10MG 113 In Stock
25MG 259 In Stock
50MG 416 In Stock
100MG 658 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    SB-435495
  • Note
    Research use only, not for human use.
  • Brief Description
    SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM.
  • Description
    SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM; inhibits the enzyme in whole human plasma with IC50 of 3 nM; shows little interaction with other CYP450 enzymes (CYP450 IC50: 1A2>100 mM, 2C9>100 uM, 2C19>40 uM, 2D6=37 uM); effectively suppresses BRB breakdown in streptozotocin-diabetic Brown Norway rats,.Atherosclerosis Phase 2 Discontinued.
  • In Vitro
    Western Blot Analysis Cell Line:oxLDL-exposed human umbilical vein endothelial cells Concentration:5 μM Incubation Time:24 hResult:The expression of Lp-PLA2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172).Cell Viability Assay 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
    ——
  • Synonyms
    SB435495
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Phospholipase
  • Recptor
    Phospholipase
  • Research Area
    Cardiovascular Disease
  • Indication
    Atherosclerosis

Chemical Information

  • CAS Number
    304694-39-1
  • Formula Weight
    720.832
  • Molecular Formula
    C38H40F4N6O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (138.73 mM)
  • SMILES
    CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C=C(C(=O)N=C3SCC4=CC=C(C=C4)F)CC5=CN(N=C5)C
  • Chemical 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]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Blackie JA, et al. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. 2. Canning P, et al. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7213-8. 3. Tyurin VA, et al. Cell Death Differ. 2014 May;21(5):825-35. 4. Jiang Z, et al. Respir Res. 2012 Nov 12;13:100.
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