SB-435495 hydrochloride
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
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- No. CAS: 304694-41-5
- Fòrmula: C38H41ClF4N6O2S
- Peso molecular:757.28
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Lp-PLA2 0.06 nM (IC50) |
SB-435495 hydrochloride inhibits CYP450 3A4 with an IC50 of 10 μM and the black membrane permeability is 0.017 cm/h[1].
SB-435495 (5 μM; 24 h) hydrochloride significantly inhibits the expression of Lp-PLA2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs[2].
SB-435495 (5 μM; 24-72 h) hydrochloride significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:oxLDL-exposed human umbilical vein endothelial cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:The expression of Lp-PLA2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172).
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Cell Line:oxLDL-exposed human umbilical vein endothelial cells
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Concentration:5 μM
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Incubation Time:24, 48 and 72 h
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Result:Significantly increased cell viability.
SB-435495 (10 mg/kg; i.p.; daily for 28 days) hydrochloride effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin (HY-13753)-diabetic Brown Norway rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:WHHL rabbit[1]
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Dosage:10 mg/kg
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Administration:Oral, once
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Result:Inhibited plasma Lp-PLA2 in the WHHL rabbit.
Chemical Information
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No. CAS 304694-41-5
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Peso molecular 757.28
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Fòrmula C38H41ClF4N6O2S
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SMILES
O=C(N(CCN(CC)CC)CC1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)CN(C(SCC3=CC=C(F)C=C3)=N4)C=C(CC5=CN(C)N=C5)C4=O.[H]Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SB-435495 hydrochloride Related Classifications
HY-19415A Related Classifications
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