SB-435495 ditartrate
SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
For research use only. We do not sell to patients.
- CAS No.: 304694-43-7
- Formula: C46H52F4N6O14S
- Molecular Weight:1021.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Phospholipase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Lp-PLA2 0.06 nM (IC50) |
In Vitro
SB-435495 ditartrate 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) ditartrate 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) ditartrate 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. Further protocols information, click here.
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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.
In Vivo
SB-435495 (10 mg/kg; i.p.; daily for 28 days) ditartrate 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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CAS No. 304694-43-7
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Molecular Weight 1021.00
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Formula C46H52F4N6O14S
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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.OC([C@H](O)[C@@H](O)C(O)=O)=O.OC([C@H](O)[C@@H](O)C(O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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 ditartrate Related Classifications
HY-19415B Related Classifications
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