PZ0406

PF-06815345

≥98% (HPLC)

• 동의어(들): (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
• 실험식(Hill 표기법): C₂₇H₂₉ClFN₉O₄·HCl
• CAS Number: 2334434-49-8
• Molecular Weight: 634.49
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: powder
• 광학 활성: [α]/D -34 to -43°, c = 0.3 in methanol
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear
• 저장 온도: 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

설명

생화학적/생리학적 작용

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.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable