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Chemical Structure : PF-06835919
CAS No.: 2102501-84-6
Catalog No.: PC-38248Not For Human Use, Lab Use Only.
PF-06835919 (PF 06835919) is a first-in-class, potent, selective Ketohexokinase (KHK) inhibitor with IC50 of 10 nM (hKHK).
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|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $548 | In stock | |
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| 100 mg | Get quote |
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PF-06835919 (PF 06835919) is a first-in-class, potent, selective Ketohexokinase (KHK) inhibitor with IC50 of 10 nM (hKHK).
PF-06835919 showed a 6-fold higher IC50 value against human KHK-A relative to human KHK-C while inhibiting rat KHK with an IC50 of 0.21 uM.
PF-06835919 exhibited a clean off-target selectivity profile as assessed by the CEREP panel at 30 uM.
Inhibition of KHK via PF-06835919 in rats prevented hyperinsulinemia and hypertriglyceridemia from fructose feeding.
PF-06835919 reversed metabolic dysfunction as rats fed the American diet developed hyperinsulinemia, hypertriglyceridemia, and hepatic steatosis.
| M.Wt | 356.349 | |
| Formula | C16H19F3N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((1R,5S,6R)-3-(2-((S)-2-methylazetidin-1-yl)-6-(trifluoromethyl)pyrimidin-4-yl)-3-azabicyclo[3.1.0]hexan-6-yl)acetic acid |
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1. Futatsugi K, et al. J Med Chem. 2020 Nov 25;63(22):13546-13560.
2. Gutierrez JA, et al. Mol Metab. 2021 Jun;48:101196.
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