For research use only. Not for therapeutic Use.
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].
PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly decreases PCSK9 protein level and increases LDLR expression in a dose dependent manner[1].
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].
| Catalog Number | I042354 |
| CAS Number | 2882035-56-3 |
| Synonyms | 7-[(3-chloro-2-fluorophenyl)methyl]-8-(2-hydroxyethylamino)-1,3-dimethylpurine-2,6-dione |
| Molecular Formula | C16H17ClFN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H17ClFN5O3/c1-21-13-12(14(25)22(2)16(21)26)23(15(20-13)19-6-7-24)8-9-4-3-5-10(17)11(9)18/h3-5,24H,6-8H2,1-2H3,(H,19,20) |
| InChIKey | UVWKWCCDYSHPMZ-UHFFFAOYSA-N |
| SMILES | CN1C2=C(C(=O)N(C1=O)C)N(C(=N2)NCCO)CC3=C(C(=CC=C3)Cl)F |
| 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. |
