Cat. No.: HY-128578

KPLH1130

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.86%
CAS No.: 906669-07-6
Formula: C₁₅H₁₃N₃O₃
Molecular Weight:283.28

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

KPLH1130 Chemical Structure

CAS No.: 906669-07-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PDK^[1]

All NO Synthase Isoforms :

All Interleukin Related Isoforms :

All HIF/HIF Prolyl-Hydroxylase Isoforms :

In Vitro

KPLH1130 (1-10 μM, 12 h) significantly reduces the mRNA expression of pro-inflammatory cytokines (TNFα, IL-6, IL-1) and the secretion of corresponding pro-inflammatory effectors in in Zymosan (HY-159069)-elicited peritoneal macrophages (ZEPMs) and LPS-elicited peritoneal macrophages (LEPMs) stimulated with LPS (HY-D1056) + IFN-γ^[1].
KPLH1130 (1-10 μM, 12 h) notably decreases the protein levels of M1 macrophage markers (HIF-1α, iNOS) and the production of nitric oxide (NO) in LPS + IFN-γ-stimulated PMs^[1].
KPLH1130 (10 μM, 3 h) prevents the reduction of basal and maximal oxygen consumption rate (OCR) in bone marrow-derived macrophages (BMDMs) induced by M1 polarization (LPS 100 ng/mL + IFN-γ 10 ng/mL), improving mitochondrial respiration function^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[1]

Cell Line:

Zymosan-elicited peritoneal macrophages (ZEPMs) and LPS-elicited peritoneal macrophages (LEPMs) stimulated with LPS (HY-D1056) + IFN-γ
Concentration:

1, 5, 10 μM
Incubation Time:

12 h
Result:

Reduced the mRNA expression of pro-inflammatory cytokines (TNFα, IL-6, IL-1) and the secretion of corresponding pro-inflammatory effectors.

In Vivo

KPLH1130 (70 mg/kg, 4 weeks) significantly improves glucose tolerance in high-fat diet (HFD)-fed C57BL/6J mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 906669-07-6
Appearance Solid
Molecular Weight 283.28
Formula C₁₅H₁₃N₃O₃
Color Off-white to gray
SMILES

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Poult Sci

ROS-mediated M1 polarization-necroptosis crosstalk involved in Di-(2-ethylhexyl) phthalate-induced chicken liver injury. [Abstract]

2025 Jan;104(1):104558. PMID: 39631278
Biol Pharm Bull

Chronic Corticosterone Treatment Decreases Extracellular pH and Increases Lactate Release via PDK4 Upregulation in Cultured Astrocytes. [Abstract]

2024;47(9):1542-1549. PMID: 39313390

Solvent & Solubility

In Vitro:

DMSO : 135 mg/mL (476.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5301 mL

17.6504 mL

35.3008 mL

5 mM

0.7060 mL

3.5301 mL

7.0602 mL

10 mM

0.3530 mL

1.7650 mL

3.5301 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (7.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5301 mL	17.6504 mL	35.3008 mL	88.2519 mL
	5 mM	0.7060 mL	3.5301 mL	7.0602 mL	17.6504 mL
	10 mM	0.3530 mL	1.7650 mL	3.5301 mL	8.8252 mL
	15 mM	0.2353 mL	1.1767 mL	2.3534 mL	5.8835 mL
	20 mM	0.1765 mL	0.8825 mL	1.7650 mL	4.4126 mL
	25 mM	0.1412 mL	0.7060 mL	1.4120 mL	3.5301 mL
	30 mM	0.1177 mL	0.5883 mL	1.1767 mL	2.9417 mL
	40 mM	0.0883 mL	0.4413 mL	0.8825 mL	2.2063 mL
	50 mM	0.0706 mL	0.3530 mL	0.7060 mL	1.7650 mL
	60 mM	0.0588 mL	0.2942 mL	0.5883 mL	1.4709 mL
	80 mM	0.0441 mL	0.2206 mL	0.4413 mL	1.1031 mL
	100 mM	0.0353 mL	0.1765 mL	0.3530 mL	0.8825 mL

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KPLH1130

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Glutamine Metabolism Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) KPLH1130

All NO Synthase Isoforms

All Interleukin Related Isoforms

All HIF/HIF Prolyl-Hydroxylase Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

KPLH1130 Related Classifications

HY-128578 Related Classifications