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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at 2-8°C,Desiccated Ships Wet ice Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA 2 inhibitor with an IC 50 of 0.06 nM
In Vitro
SB-435495 inhibits CYP450 3A4 with an IC 50 of 10 μM and the black membrane permeability is 0.017 cm/h. SB-435495 (5 μM; 24 h) significantly inhibits the expression of Lp-PLA 2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs. SB-435495 (5 μM; 24-72 h) significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: oxLDL-exposed human umbilical vein endothelial cells Concentration: 5 μM Incubation Time: 24 h Result: The expression of Lp-PLA 2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172). Cell Viability AssayCell 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) inhibits plasma Lp-PLA 2 in the WHHL rabbit . SB-435495 (10 mg/kg; i.p.; daily for 28 days) effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin -diabetic Brown Norway rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Lp-PLA2 0.06 nM (IC 50 )
| Sorrisos canónicos | 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 |
|---|---|
| SMILES isoméricas | 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 |
| PubChem CID | 10417440 |
| Peso molecular | 720.82 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Solubilidade | DMSO : 100 mg/mL (138.73 mM; Need ultrasonic) |
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| Peso molecular | 720.800 g/mol |
| XLogP3 | 6.500 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 15 |
| Exact Mass | 720.287 Da |
| Monoisotopic Mass | 720.287 Da |
| Topological Polar Surface Area | 99.300 Ų |
| Heavy Atom Count | 51 |
| Formal Charge | 0 |
| Complexity | 1190.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |