PF-06815345 

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: >20 μM (cell based), 13.4 (cell free) for Proprotein convertase subtilisin/kexin type 9 (PCSK9)^[2]

PF-06815345 (Example 7) (1-30 μM; 5-1440 min) in human enterocyte and hepatocyte with CL_int values of <82.9 μL/min/mg and 97.6 μL/min/mg, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

598.03

C₂₇H₂₉ClFN₉O₄

1900686-46-5

O=C(N([C@H]1CNCCC1)C2=C(Cl)C=CC=N2)C3=CC=C(C4=C(C5=NN=NN5[C@H](C)OC(OCC)=O)N(C)N=C4)C(F)=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.