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| Targets |
TXNIP-IN-1 targets the thioredoxin-interacting protein (TXNIP)-thioredoxin (TRX) complex. TXNIP is a key regulator of oxidative stress, glucose homeostasis, and inflammatory signaling. By inhibiting the TXNIP-TRX complex, the compound modulates these pathways. It targets TXNIP mRNA in human pancreatic islets.
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| ln Vitro |
High glucose (HG-sensing) TXNIP-TRX complex formation is inhibited by TXNIP-IN-1 [1]. In monocytes, TXNIP-IN-1 (1.25–5 μM) and HG cause TNF expression [1]. TXNIP mRNA expression is inhibited in THP1 cells by IN-1 (1.25-5 μM; 72 hours) [1]. TXNIP-IN-1 (0.3–10 μM; 72 hours) prevents RAW macrophages from expressing TXNIP mRNA. In MIN6 cells, TXNIP-IN-1 (5–20 μM; 72 hours) lowers TXNIP but not TNF-α mRNA levels [1]. In human pancreatic 1.1B4 β-cells, TXNIP-IN-1 (0.62-5 μM; 72 hours) influences the expression of TXNIP and TNF-α mRNA [1]. In cultivated THP1 cells, TXNIP-IN-1 (5 μM; 16–72 hours) suppresses c-TRX responsiveness at a concentration of 25 mM [1]. In human pancreatic islets, TXNIP-IN-1 suppresses TXNIP mRNA [1].
In vitro, TXNIP-IN-1 is a potent small-molecule inhibitor of the TXNIP-TRX complex. It is an inhibitor of TXNIP mRNA in human pancreatic islets. The compound's activity is assessed by measuring its ability to inhibit TXNIP-TRX complex formation and modulate downstream signaling pathways. It is used in research on diabetes, cardiovascular disease, and inflammatory diseases. |
| ln Vivo |
In vivo, TXNIP-IN-1 is used in research on TXNIP-TRX complex associated metabolic disorders (diabetes), cardiovascular disease, or inflammatory disease. Its ability to modulate oxidative stress, glucose homeostasis, and inflammatory signaling makes it a valuable tool for studying these diseases. Further in vivo studies are needed to evaluate its therapeutic potential.
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| Enzyme Assay |
In vitro binding assays for TXNIP-IN-1 measure its ability to inhibit the TXNIP-TRX complex formation. Surface plasmon resonance (SPR) or fluorescence polarization assays can be used to measure binding affinity. The compound's ability to disrupt the TXNIP-TRX interaction is assessed. TXNIP mRNA levels are measured by qRT-PCR in human pancreatic islets.
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| Cell Assay |
In vitro cellular studies are conducted using pancreatic islets or other cell types. Cells are treated with TXNIP-IN-1 at various concentrations. TXNIP mRNA levels are measured by qRT-PCR. TXNIP protein levels and TRX activity are measured by Western blot or enzymatic assays. Oxidative stress markers, glucose uptake, and inflammatory cytokine production are assessed. Cell viability is assessed using standard cytotoxicity assays.
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| Animal Protocol |
In vivo animal experiments are performed in models of diabetes, cardiovascular disease, or inflammatory disease. Animals are administered TXNIP-IN-1 via various routes at different doses. Blood glucose levels, insulin sensitivity, and inflammatory markers are measured. Tissue samples are collected for analysis of TXNIP expression, oxidative stress, and signaling pathways.
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| ADME/Pharmacokinetics |
TXNIP-IN-1 has a molecular formula of C12H12N2O4 and a molecular weight that corresponds to its structure. It is an inhibitor of the TXNIP-TRX complex. For storage, it should be kept at -20°C, protected from light and moisture. The compound is supplied with high purity (≥98%) for research purposes. It is extracted from patent US20200085800A1, Compound 1.
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| Toxicity/Toxicokinetics |
As a research chemical with potent biological activity, TXNIP-IN-1 is not intended for human use. Its toxicological profile is not fully characterized. Standard laboratory safety precautions should be followed when handling it. Its effects are related to its mechanism as a TXNIP-TRX complex inhibitor, which could have significant effects on metabolism and inflammation.
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| References | |
| Additional Infomation |
TXNIP-IN-1 is an inhibitor of the thioredoxin-interacting protein (TXNIP)-thioredoxin (TRX) complex. It targets TXNIP mRNA in human pancreatic islets. The compound is used in the research of TXNIP-TRX complex associated metabolic disorders (diabetes), cardiovascular disease, or inflammatory disease. It is extracted from patent US20200085800A1, Compound 1.
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| Molecular Formula |
C12H12N2O4
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|---|---|
| Molecular Weight |
248.234683036804
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| Exact Mass |
248.079
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| CAS # |
1268955-50-5
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| Related CAS # |
(S)-TXNIP-IN-1;1212421-96-9
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| PubChem CID |
47001822
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| Appearance |
White to light yellow solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
394
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(C(C(C)C)N1C(C2C=NC=CC=2C1=O)=O)=O
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| InChi Key |
KTDYLXVLROCGRL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N2O4/c1-6(2)9(12(17)18)14-10(15)7-3-4-13-5-8(7)11(14)16/h3-6,9H,1-2H3,(H,17,18)
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| Chemical Name |
2-(1,3-dioxopyrrolo[3,4-c]pyridin-2-yl)-3-methylbutanoic acid
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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 : ~50 mg/mL (~201.43 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.07 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 (10.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0285 mL | 20.1426 mL | 40.2852 mL | |
| 5 mM | 0.8057 mL | 4.0285 mL | 8.0570 mL | |
| 10 mM | 0.4029 mL | 2.0143 mL | 4.0285 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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