PZ0406

PF-06815345

≥98% (HPLC)

• Synonyma: (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
• Empirický vzorec (Hillův zápis): C₂₇H₂₉ClFN₉O₄·HCl
• Číslo CAS: 2334434-49-8
• Molekulová hmotnost: 634.49
• UNSPSC Code: 12352200
• NACRES: NA.77

Vlastnosti

• 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
• 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

Popis

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.

Bezpečnostní informace

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable