| Identification | Back Directory | [Name]
PF-06815345 | [CAS]
1900686-46-5 | [Synonyms]
MDK6465
PF 6815345
PF-06815345
Carbonic acid, (1S)-1-[5-[4-[4-[[(3-chloro-2-pyridinyl)(3R)-3-piperidinylamino]carbonyl]-2-fluorophenyl]-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl]ethyl ethyl ester | [Molecular Formula]
C27H29ClFN9O4 | [MOL File]
1900686-46-5.mol | [Molecular Weight]
598.03 |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
| [References]
[1] Akin A, et al. Overcoming the Challenges of Making a Single Enantiomer N-1 Substituted Tetrazole Prodrug Using a Tin-Mediated Alkylation and Enzymatic Resolution[J]. Organic Process Research & Development, 2019, 23(6): 1167-1177.
[2] Darout E, et al. Preparation of substituted amide compounds as PCSK9 inhibitors: Canada, CA2907071 A1 2016-04-08. |
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