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SB-435495

Chemical Structure : SB-435495

CAS No.: 304694-39-1

SB-435495 (SB435495)

Catalog No.: PC-63003Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 720.832
Formula C38H40F4N6O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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]-

References

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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