| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
ThioLox responds to the active site of 15-LOX-1 non-covalently by exhibiting competitive inhibition [1]. In precision-cut lung slices (PCLS), ThioLox (50 μM; 24 h) reduces interleukin (IL). In neuronal cells, ThioLox (10 μM; 16 h) inhibits mitochondrial peroxidation and mitochondrial superoxide expression [1]. ThioLox (5–20 μM; 14–16 h) dramatically lowers neuronal cell death while shielding HT-22 cell scaffolds from glutathione toxicity[1].
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|---|---|
| ln Vivo |
ThioLox has a logP value of 3 and the measured numerical predictive power crosses the blood-brain barrier [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: Precision- Formation[1]. Lung Sections (PCLS) Tested Concentrations: 1, 5, 10, 25 and 50 μM Incubation Duration: 20 hrs (hours) mixed with 10 μM linoleic acid and stimulated with 10 ng/mL LPS for the last 4 hrs (hours). Experimental Results: At 50 μM, the pro-inflammatory gene IL- The expression of 1β, IL-6, IL-8, IL-12b, TNFα and iNOS was inhibited by nearly 50%. Cell viability assay[1] Cell Types: Neuronal HT-22 Cell Tested Concentrations: 5, 10 and 20 μM Incubation Duration: 14-16 hrs (hours) Experimental Results: Neuronal cell death was Dramatically diminished in response to glutamate toxicity. |
| References |
[1]. Eleftheriadis N, et al. Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties. Eur J Med Chem. 2016 Oct 21;122:786-801.
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| Molecular Formula |
C15H18N2OS
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|---|---|
| Molecular Weight |
274.382
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| Exact Mass |
274.11
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| Elemental Analysis |
C, 65.66; H, 6.61; N, 10.21; O, 5.83; S, 11.68
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| CAS # |
1202193-89-2
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(C1=C(N)SC(C2=CC=CC=C2)=C1)NCCCC
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| InChi Key |
QWWMJRJCSZMXHZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H18N2OS/c1-2-3-9-17-15(18)12-10-13(19-14(12)16)11-7-5-4-6-8-11/h4-8,10H,2-3,9,16H2,1H3,(H,17,18)
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| Chemical Name |
2-amino-N-butyl-5-phenylthiophene-3-carboxamide
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| Synonyms |
ThioLox,
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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 : ~100 mg/mL (~364.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.11 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 (9.11 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 | 3.6446 mL | 18.2229 mL | 36.4458 mL | |
| 5 mM | 0.7289 mL | 3.6446 mL | 7.2892 mL | |
| 10 mM | 0.3645 mL | 1.8223 mL | 3.6446 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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