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About This Item
Empirical Formula (Hill Notation):
C27H29ClFN9O4·HCl
CAS Number:
Molecular Weight:
634.49
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
SMILES string
Fc1c(ccc(c1)C(=O)N([C@H]5CNCCC5)c4ncccc4Cl)c2c([n](nc2)C)c3[n](nnn3)[C@@H](OC(=O)OCC)C.Cl
InChI key
RFEUFHPTEFEGDQ-KUGOCAJQSA-N
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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