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PZ0406

Sigma-Aldrich

PF-06815345

≥98% (HPLC)

Synonym(s):

(1S)-1-(5-(4-(4-((3-Chloropyridin-2-yl)((R)-piperidin-3-yl)carbamoyl)-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl)-1H-tetrazol-1-yl)ethyl ethyl carbonate hydrochloride, Ethyl (S)-1-{5-[4-(4-{(3-chloropyridin-2-yl)[(3R)-piperidin-3-yl]carbamoyl}-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl}ethyl carbonate hydrochloride, PF 06815345, PF06815345

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About This Item

Empirical Formula (Hill Notation):
C27H29ClFN9O4·HCl
CAS Number:
2334434-49-8
Molecular Weight:
634.49
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -34 to -43°, c = 0.3 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

Biochem/physiol Actions

PF-06815345 is a liver-targeted, orally available prodrug, which is converted by liver carboxyesterase (CES1) to its zwitterionic active drug (liver active drug = 33.9 μg/mL in mice 0.5 hr post 300 mg/kg p.o. and 9.0 μg/mL in monkeys 0.5 hr post 30 mg/kg p.o.) that selectively inhibits PCSK9 protein synthesis (IC50 = 3.7 μM by in vitro hPCSK9 translation; 4.95/3.81/21/24/>27-fold selective over CDH1/HSD17B11/PCBP2/RPL27/BCAP31). PF-06815345 effectively lowers plasma PCSK9 in humanized PCSK9 mice (by 26/42/53% 5 hrs post 100/300/500 mg/kg p.o.) and is well tolerated in rats and monkeys in vivo. Note: PF-06815345 is not active in non-humanized mice.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Kim F McClure et al.
Angewandte Chemie (International ed. in English), 56(51), 16218-16222 (2017-10-27)
Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. A liver-targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9, a lipid regulator considered undruggable by small molecules. Key to the concept was

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