PF-06815345
CAS No. : 1900686-46-5
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| Cat. No. : | HY-112598 |
| M.Wt: | 598.03 |
| Formula: | C27H29ClFN9O4 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
PF-06815345 is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 significantly decreases the PCSK9 level in vivo in mouse[1][2].
IC50 & Target:IC50: >20 μM (cell based), 13.4 (cell free) for Proprotein convertase subtilisin/kexin type 9 (PCSK9)[2]
In Vitro:PF-06815345 (Example 7) (1-30 μM; 5-1440 min) in human enterocyte and hepatocyte with CLint values of <82.9 μL/min/mg and 97.6 μL/min/mg, respectively[2].
In Vivo:PF-06815345 (Example 7) (100-500 mg/kg; p.o; single dose) lowers the level of PCSK9 in humanized PCSK9 mouse model. It lowers plasma PCSK9 to 72% at 500 mg/kg 4 hr later treatment[2].
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