| Identification | Back Directory | [Name]
8-(2-methoxyethylamino)-7-[(3-methoxyphenyl)methyl]-1,3-dimethylpurine-2,6-dione | [CAS]
368434-98-4 | [Synonyms]
PCSK9-IN-10
8-(2-methoxyethylamino)-7-[(3-methoxyphenyl)methyl]-1,3-dimethylpurine-2,6-dione
7-(3-Methoxybenzyl)-8-((2-methoxyethyl)amino)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
1H-Purine-2,6-dione, 3,7-dihydro-8-[(2-methoxyethyl)amino]-7-[(3-methoxyphenyl)methyl]-1,3-dimethyl- | [Molecular Formula]
C18H23N5O4 | [MOL File]
368434-98-4.mol | [Molecular Weight]
373.41 |
| Chemical Properties | Back Directory | [Boiling point ]
581.1±60.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.33±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PCSK9-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[1]. | [in vivo]
PCSK9-IN-10 (30 mg/kg; p.o.; once a day for 8 weeks) reduces total cholesterol (TC) and atherosclerotic plaque size in ApoE KO mice[1]. | Animal Model: | Eight weeks old male ApoE KO mice[1] | | Dosage: | 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. |
| [References]
[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. DOI:10.1016/j.ejmech.2022.115047 |
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