PF-06835919 | Ketohexokinase inhibitor | Probechem Biochemicals

Chemical Structure : PF-06835919

CAS No.: 2102501-84-6

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PF-06835919 (PF06835919)

货号: 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	￥3580	In stock
10 mg	￥5480	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	356.349
分子式	C16H19F3N4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

PF-06835919 (PF06835919)

生物&药学活性

物理化学性质&存储条件

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PF-06835919 (PF06835919)

生物&药学活性

物理化学性质&存储条件

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