For research use only. Not for therapeutic Use.
PF-06815345 hydrochloride 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 hydrochloride significantly decreases the PCSK9 level in vivo in mouse[1][2].
PF-06815345 hydrochloride (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].
PF-06815345 hydrochloride (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].
Catalog Number | I041828 |
CAS Number | 2334434-49-8 |
Synonyms | [(1S)-1-[5-[4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]-2-fluorophenyl]-2-methylpyrazol-3-yl]tetrazol-1-yl]ethyl] ethyl carbonate;hydrochloride |
Molecular Formula | C27H30Cl2FN9O4 |
Purity | ≥95% |
InChI | InChI=1S/C27H29ClFN9O4.ClH/c1-4-41-27(40)42-16(2)38-25(33-34-35-38)23-20(15-32-36(23)3)19-10-9-17(13-22(19)29)26(39)37(18-7-5-11-30-14-18)24-21(28)8-6-12-31-24;/h6,8-10,12-13,15-16,18,30H,4-5,7,11,14H2,1-3H3;1H/t16-,18+;/m0./s1 |
InChIKey | RFEUFHPTEFEGDQ-KUGOCAJQSA-N |
SMILES | CCOC(=O)OC(C)N1C(=NN=N1)C2=C(C=NN2C)C3=C(C=C(C=C3)C(=O)N(C4CCCNC4)C5=C(C=CC=N5)Cl)F.Cl |
Reference | [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. |