| Identification | Back Directory | [Name]
PDK4-IN-1 | [CAS]
2310262-10-1 | [Synonyms]
PDK4-IN-1
9,10-Anthracenedione, 1-[1-(4-piperidinyl)-1H-pyrazol-4-yl]- | [Molecular Formula]
C22H19N3O2 | [MDL Number]
MFCD34470081 | [MOL File]
2310262-10-1.mol | [Molecular Weight]
357.41 |
| Chemical Properties | Back Directory | [Boiling point ]
620.6±55.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.83±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1]. | [in vivo]
PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance[1].
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs[1].
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats[1]. | Animal Model: | C57BL/6J mice (8-week old) fed with high-fat diet[1] | | Dosage: | 100 mg/kg | | Administration: | Oral administration; daily; for 1 week | | Result: | Significantly improved glucose tolerance.
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| [References]
[1] Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588. DOI:10.1021/acs.jmedchem.8b01168 |
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