2310262-10-1

Name	PDK4-IN-1
CAS	2310262-10-1
Molecular Formula	C22H19N3O2
MDL Number	MFCD34470081
Molecular Weight	357.41
MOL File	2310262-10-1.mol

Synonyms

PDK4-IN-1 9,10-Anthracenedione, 1-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-

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Chemical Properties

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

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.

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

Supplier

Shanghai Rechem science Co., Ltd.

Telephone021-31433387 15618786686

Websitehttp://cn.rechemscience.com

Hubei wei shi reagent group ltd., company

Telephone027-59102966 18717199209

Websitehttps://www.4008081911.com

Shanghai Maclean Biochemical Technology Co., LTD

Telephone021-50706066 15221275939

Websitehttp://www.macklin.cn/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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