PF-06835919 is an oral Class I clinical candidate for NAFLD/NASH, targeting ketohexokinase (KHK), an enzyme that initiates fructose metabolism.
| Molecular Weight | 356.35 |
| Formula | C16H19F3N4O2 |
| CAS Number | 2102501-84-6 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Suzanna L Attia, et al. Clin Transl Sci. Evolving Role for Pharmacotherapy in NAFLD/NASH
| Related Ketohexokinase Products |
|---|
| KHK-IN-3
KHK-IN-3 is a ketohexokinase (KHK) inhibitor. |
| KHK-IN-2
KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM. |
| KHK-IN-1 hydrochloride
KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity. |
| KHK-IN-1
KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity. |
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