| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
KPLH1130 targets pyruvate dehydrogenase kinase (PDK), a key enzyme that regulates the balance between glycolysis and oxidative phosphorylation. By inhibiting PDK, it activates the pyruvate dehydrogenase complex (PDC), which converts pyruvate to acetyl-CoA, promoting glucose oxidation and reducing lactate production. This metabolic shift has anti-inflammatory effects, particularly on macrophages.
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| ln Vitro |
In vitro, 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 reducing nitric oxide (NO) production. This indicates that PDK inhibition can attenuate pro-inflammatory responses in macrophages.
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| ln Vivo |
In vivo, KPLH1130 enhances glucose tolerance in mice fed a high-fat diet (HFD). It improves glucose tolerance and insulin sensitivity in metabolic disease models. Its ability to block macrophage polarization and reduce inflammatory responses suggests it has potential for treating obesity-related inflammation and diabetes.
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| Enzyme Assay |
The in vitro PDK enzyme assay for KPLH1130 involves measuring its ability to inhibit PDK activity. The enzyme is incubated with a substrate, such as pyruvate dehydrogenase (E1), and ATP in the presence of varying concentrations of the compound. The phosphorylation of E1 is measured, and the IC50 is calculated from the inhibition curve.
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| Cell Assay |
In vitro cell culture studies for KPLH1130 utilize macrophages. Cells are treated with the compound and stimulated with LPS to induce M1 polarization. The expression of M1 markers (HIF-1α, iNOS) and pro-inflammatory cytokines (TNF-α, IL-6) is measured by qPCR or ELISA. Nitric oxide production is measured using the Griess reagent.
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| Animal Protocol |
In vivo animal experiments for KPLH1130 are performed in mice fed a high-fat diet (HFD). The compound is administered orally, and glucose tolerance is assessed by an oral glucose tolerance test (OGTT). Insulin sensitivity is measured by an insulin tolerance test (ITT). Inflammatory markers in adipose tissue and serum are measured by ELISA.
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| ADME/Pharmacokinetics |
KPLH1130 has a molecular formula of C15H13N3O3 and a molecular weight of 283.28 g/mol. It is a solid compound that is soluble in DMSO. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for KPLH1130 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
KPLH1130 is a research compound with no clinical approval. It is a valuable tool for studying the role of PDK in metabolism and inflammation. It is used in drug discovery programs to explore the therapeutic potential of PDK inhibitors for the treatment of metabolic diseases, such as type 2 diabetes and obesity, as well as inflammatory disorders.
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| Molecular Formula |
C15H13N3O3
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|---|---|
| Molecular Weight |
283.282023191452
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| Exact Mass |
283.095
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| CAS # |
906669-07-6
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| PubChem CID |
135487465
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| Appearance |
Off-white to gray solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
432
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C2C=CC(C)=CC=2)C(C2C(O)=CC(O)=CC=2)=NN1
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| InChi Key |
UUTBMTOBGXJTLN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13N3O3/c1-9-2-4-10(5-3-9)18-14(16-17-15(18)21)12-7-6-11(19)8-13(12)20/h2-8,19-20H,1H3,(H,17,21)
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| Chemical Name |
3-(2,4-dihydroxyphenyl)-4-(4-methylphenyl)-1H-1,2,4-triazol-5-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~135 mg/mL (~476.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (7.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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