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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C16H19F3N4O3
CAS Number:
2135304-43-5
Molecular Weight:
372.34
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD31813616

Key Documents

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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000141321
0000141322
0000123184

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