KPLH1130

KPLH1130 is a pyruvate dehydrogenase kinase (PDK) inhibitor. KPLH1130 potently inhibits M1 macrophage polarization by reducing the expression of pro-inflammatory cytokines, decreasing the levels of M1 phenotype markers (HIF-1α, iNOS) and nitric oxide (NO) production. KPLH1130 prevents the reduction of mitochondrial oxygen consumption rate (OCR) induced by inflammatory stimuli (LPS ((HY-D1056) + IFN-γ) in various macrophage types. KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 can be used for the study of obesity-associated metabolic disorders and other inflammatory conditions[1].

Product Specifications

CAS Number

[906669-07-6]

UNSPSC

12352005

Target

HIF/HIF Prolyl-Hydroxylase; Interleukin Related; NO Synthase; PDHK

Type

Reference compound

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/kplh1130.html

Purity

99.86

Solubility

DMSO : 135 mg/mL (ultrasonic)

Smiles

OC1=CC=C(C2=NNC(N2C3=CC=C(C)C=C3)=O)C(O)=C1

Molecular Formula

C15H13N3O3

Molecular Weight

283.28

References & Citations

[1]Min BK, et al. Pyruvate Dehydrogenase Kinase Is a Metabolic Checkpoint for Polarization of Macrophages to the M1 Phenotype. Front Immunol. 2019 May 7;10:944.