| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Targets |
Microsomal triglyceride transfer protein (MTP), also known as MTTP. KD-026 is a potent, selective, and orally active enterocytic MTP inhibitor with an IC50 of 8.0 nM. MTP is a protein that plays a crucial role in the production of chylomicrons, which are used to transport triglycerides and cholesterol into the systemic circulation. KD-026 acts selectively in the enterocytes lining the gastrointestinal tract, preventing the formation of chylomicrons. This enterocyte-specific action distinguishes it from first-generation MTP inhibitors that inhibit both hepatic and intestinal MTP.
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| ln Vitro |
In Caco-2 cells, SLX-4090 suppresses the production of apolipoprotein B (IC50 value of 9.6 nM) but not apolipoprotein A1 [1].
KD-026 is a potent MTP inhibitor with an IC50 of 8.0 nM. In Caco-2 cells, KD-026 suppresses the production of apolipoprotein B with an IC50 value of 9.6 nM but does not affect apolipoprotein A1 secretion. This indicates selective inhibition of the apolipoprotein B-containing lipoprotein assembly pathway, which is dependent on MTP activity. The compound's enterocyte-specific action allows it to inhibit MTP localized to enterocytes. |
| ln Vivo |
SLX-4090 (oral dose, 30 mg/kg) can 50% lower postprandial blood lipids in rats, with an ED50 value of 7 mg/kg[1].
In vivo, KD-026 (oral dose, 30 mg/kg) can lower postprandial blood lipids by 50% in rats, with an ED50 value of 7 mg/kg. This demonstrates significant in vivo efficacy in reducing postprandial lipid levels. The compound is being investigated for use and treatment in hyperlipidemia and type 2 diabetes. Its enterocyte-specific action reduces systemic exposure and potential hepatic toxicity compared to non-selective MTP inhibitors. |
| Enzyme Assay |
In vitro enzyme inhibition assays for KD-026 involve measuring the activity of microsomal triglyceride transfer protein (MTP) in the presence of varying concentrations of the compound. The enzyme is incubated with lipid substrates, and the transfer of triglycerides between donor and acceptor vesicles is quantified. The IC50 value of 8.0 nM is determined from the dose-response curve. Selectivity for enterocytic MTP over hepatic MTP can also be assessed.
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| Cell Assay |
In vitro cell-based assays for KD-026 assess its effects on MTP-dependent lipoprotein assembly in Caco-2 cells, a human intestinal epithelial cell line. Cells are treated with KD-026, and the production of apolipoprotein B is measured. The compound suppresses apolipoprotein B production with an IC50 value of 9.6 nM but does not affect apolipoprotein A1 secretion. This demonstrates selective inhibition of the chylomicron assembly pathway.
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| Animal Protocol |
In vivo studies of KD-026 have been conducted in rat models. The compound is administered orally, and its effects on postprandial blood lipids are measured. At an oral dose of 30 mg/kg, KD-026 lowers postprandial blood lipids by 50%, with an ED50 value of 7 mg/kg. These studies demonstrate the compound's efficacy in reducing postprandial lipid levels. The compound is soluble in DMSO at 55 mg/mL.
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| ADME/Pharmacokinetics |
KD-026 is orally bioactive and administered orally. The compound has a molecular weight of 546.54, a LogP of 6.78, and is soluble in DMSO at 55 mg/mL (100.63 mM). It is typically stored as a powder at -20°C for long-term stability. Detailed pharmacokinetic parameters such as half-life, Cmax, and AUC are available from primary literature but are not extensively detailed in the available sources.
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| Toxicity/Toxicokinetics |
Specific toxicological data for KD-026 are not detailed in the available literature. As an investigational compound, its safety profile has been evaluated in preclinical studies. The enterocyte-specific action of KD-026 is designed to reduce systemic exposure and potential hepatic toxicity compared to first-generation MTP inhibitors that inhibit both hepatic and intestinal MTP. The compound is for research use only and is not for human use.
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| References |
[1]. Enoch Kim, et al. A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85.
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| Additional Infomation |
SLx-4090 is a microsomal triglyceride transfer protein (MTTP) inhibitor with potential for the treatment of type 2 diabetes.
Drug Indications It has been investigated for the treatment of hyperlipidemia. Mechanism of Action SLx-4090 inhibits microsomal triglyceride transfer protein (MTP). It selectively acts on intestinal cells in the lining of the gastrointestinal tract, preventing the formation of chylomicrons, which are responsible for transporting triglycerides (TG) and cholesterol into the systemic circulation. KD-026 is a research tool for studying MTP function and lipid metabolism. It is an investigational, orally active small-molecule inhibitor of MTP that selectively targets MTP in intestinal enterocytes. The compound may be utilized in the research and study of dyslipidemia and type 2 diabetes. KD-026 is also known as SLx-4090 or SLX-4090. It is not an approved therapeutic agent. |
| Molecular Formula |
C31H25F3N2O4
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|---|---|
| Molecular Weight |
546.54
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| Exact Mass |
546.176
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| CAS # |
913541-47-6
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| Related CAS # |
913541-44-3 (metabolite);913541-47-6;
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| PubChem CID |
53497429
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
593.8±50.0 °C at 760 mmHg
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| Flash Point |
312.9±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.614
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| LogP |
6.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
856
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCC2C(=CC=C(NC(C3C(C4C=CC(C(F)(F)F)=CC=4)=C(OC)C=CC=3)=O)C=2)C1)OC1C=CC=CC=1
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| InChi Key |
AZUIUVJESCFSLJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H25F3N2O4/c1-39-27-9-5-8-26(28(27)20-10-13-23(14-11-20)31(32,33)34)29(37)35-24-15-12-22-19-36(17-16-21(22)18-24)30(38)40-25-6-3-2-4-7-25/h2-15,18H,16-17,19H2,1H3,(H,35,37)
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| Chemical Name |
phenyl 6-[[3-methoxy-2-[4-(trifluoromethyl)phenyl]benzoyl]amino]-3,4-dihydro-1H-isoquinoline-2-carboxylate
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| Synonyms |
KD026; SLx-4090; KD-026
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~182.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8297 mL | 9.1485 mL | 18.2969 mL | |
| 5 mM | 0.3659 mL | 1.8297 mL | 3.6594 mL | |
| 10 mM | 0.1830 mL | 0.9148 mL | 1.8297 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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