| Chemical Properties | Back Directory | [Boiling point ]
607.3±65.0 °C(predicted) | [density ]
1.53±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
14.54±0.10(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research[1]. | [in vivo]
PCSK9-IN-11 (compound 5r) (0-1000 mg/kg, IG, once) exhibits a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg[1].
PCSK9-IN-11 (30 mg/kg, IG, once a day for 8 weeks) significantly suppresses hepatic PCSK9 expression and slightly reduces serum PCSK9 level[1].
| Animal Model: | C57BL/6J mice[1] | | Dosage: | 0, 250, 500 or 1000 mg/kg | | Administration: | Intragastrically administrated, single dose | | Result: | Exhibited a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg. Did not affected the body weight, behavioral and survival characteristics of mice. |
| Animal Model: | ApoE KO mice (under high-fat diet (HFD))[1] | | Dosage: | 30 mg/kg | | Administration: | Intragastric administration, once a day for 8 weeks | | Result: | Significantly suppressed hepatic PCSK9 expression and slightly reduced serum PCSK9 level. |
| [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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