
PCSK9-IN-10
CAS No. 368434-98-4
PCSK9-IN-10( —— )
Catalog No. M36396 CAS No. 368434-98-4
PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 μM.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 62 | Get Quote |
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5MG | 92 | Get Quote |
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10MG | 147 | Get Quote |
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25MG | 288 | Get Quote |
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50MG | 454 | Get Quote |
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100MG | 653 | Get Quote |
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500MG | 1368 | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NamePCSK9-IN-10
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NoteResearch use only, not for human use.
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Brief DescriptionPCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 μM.
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DescriptionPCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 μM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.
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In VitroCell Cytotoxicity Assay Cell Line:HepG2 cells Concentration:0-1000 μM Incubation Time:24 h Result:Showed low cytotoxicity to HepG2 cells.Western Blot Analysis Cell Line:HepG2 cells Concentration:0, 2.5, 5, 12.5, 25 μM Incubation Time:24 h Result:Significantly decreased PCSK9 protein level in a dose dependent manner.
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In VivoAnimal Model:Eight weeks old male ApoE KO miceDosage:30 mg/kg Administration:P.o.; once a day for 8 weeks Result:Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size.
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Synonyms——
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PathwayApoptosis
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TargetSerine/threonin kinase
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RecptorSerine/threonin kinase
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Research Area——
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Indication——
Chemical Information
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CAS Number368434-98-4
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Formula Weight373.41
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Molecular FormulaC18H23N5O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 250 mg/mL (669.51 mM; Ultrasonic )
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SMILESCOCCNc1nc2n(C)c(=O)n(C)c(=O)c2n1Cc1cccc(OC)c1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047.?
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