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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 |
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| 5MG | 70 | In Stock |
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| 10MG | 113 | In Stock |
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| 25MG | 259 | In Stock |
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| 50MG | 416 | In Stock |
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| 100MG | 658 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameSB-435495
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NoteResearch use only, not for human use.
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Brief DescriptionSB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM.
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DescriptionSB-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.
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In VitroWestern 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.
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In Vivo——
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SynonymsSB435495
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PathwayMetabolic Enzyme/Protease
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TargetPhospholipase
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RecptorPhospholipase
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Research AreaCardiovascular Disease
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IndicationAtherosclerosis
Chemical Information
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CAS Number304694-39-1
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Formula Weight720.832
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Molecular FormulaC38H40F4N6O2S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (138.73 mM)
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SMILESCCN(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
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Chemical Name1(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
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Melittin TFA(20449-7...
Melittin TFA is a small protein containing 26 amino acid residues, is the principal toxic component of bee venom. Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2.Melittin, an immunologically related PLA2 stimulating peptide from bee venom, increases the activity of the high molecular weight enzyme.
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MAFP
MAFP (Methyl Arachidonyl Fluorophosphonate) is an effective, active-site directed irreversible inhibitor of anandamide amidase, cPLA2, and iPLA2.
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Bromoenol lactone
Bromoenol lactone ((6E)-Bromoenol lactone) is a selective calcium-dependent phospholipase A2?(iPLA2β) and serine protease inhibitor that attenuates nicotine-induced breast cancer cell proliferation and migrations.
