PZ0417

PF-06752469

≥98% (HPLC)

• Synonym(s): 6-((3S,4S)-3,4-Dihydroxypyrrolidin-1-yl)-2-((S)-3-hydroxy-3-methylpyrrolidin-1-yl)-4-(trifluoromethyl)nicotinonitrile, 6-[(3S,4S)-3,4-Dihydroxy-1-pyrrolidinyl]-2-[(3S)-3-hydroxy-3-methyl-1-pyrrolidinyl]-4-(trifluoromethyl)-3-pyridinecarbonitrile, KHK-IN-2, PF 06752469, PF 675, PF 6752469, PF-675, PF-6752469, PF06752469, PF675, PF6752469
• Empirical Formula (Hill Notation): C₁₆H₁₉F₃N₄O₃
• CAS Number: 2135304-43-5
• Molecular Weight: 372.34
• MDL number: MFCD31813616
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

PF-06752469 (PF-6752469) is an orally active, non-cytotoxic (300 μM, HepG2), potent and selective ketohexokinase (KHK) inhibitor (human KHK-A/C IC50 = 390/450 nM; rat KHK IC50 = 340 nM) with no significant activity against a broad panel of transporters, receptors, ion channels, and enzymes, including hERG and human CYP450s. PF-06752469 prevents fructose administration-induced fructose 1-phosphate (F1P) upregulation (hepatic/renal ED50 = 15.7/30.0 mg/kg p.o. 2 min prior to 500 mg fructose/10 mL/kg i.v. in rats) by inhibiting KHK-mediated fructose metabolism in vivo.

Safety Information

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