Tigulixostat
Based on 1 publication(s) in Google Scholar
Tigulixostat (LC350189) is an orally active non-purine selective xanthine oxidase inhibitor. Tigulixostat has IC50 values of 0.003 µM and 0.073 µM in bovine milk and rat plasma, respectively. Tigulixostat can effectively reduce serum uric acid levels and can be used in the research of gout and hyperuricemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.18%
- No. CAS: 1287766-55-5
- Fòrmula: C16H14N4O2
- Peso molecular:294.31
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tigulixostat
More
Actividad biológica
Descripciòn
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1287766-55-5
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Appearance Solid
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Peso molecular 294.31
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Fòrmula C16H14N4O2
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Color White to light yellow
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SMILES
N#CC1=CN(C(C)C)C2=C1C=C(N3N=CC(C(O)=O)=C3)C=C2
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Synonyms
LC350189
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (339.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Seonghae Yoon, et al. Pharmacokinetics, pharmacodynamics, and tolerability of LC350189, a novel xanthine oxidase inhibitor, in healthy subjects. Drug Des Devel Ther. 2015 Aug 31;9:5033-49. [Content Brief]
[2]. Terkeltaub R, et al. Serum Urate-Lowering Efficacy and Safety of Tigulixostat in Gout Patients With Hyperuricemia: A Randomized, Double-Blind, Placebo-Controlled, Dose-Finding Trial. Arthritis Rheumatol. 2023 Jul;75(7):1275-1284. [Content Brief]
[3]. Xue L, et al. Tigulixostat Alleviates Hyperuricemic Nephropathy by Promoting M2 Macrophage Polarization. J Inflamm Res. 2025 Jan 3;18:17-30. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3978 mL | 16.9889 mL | 33.9778 mL | 84.9444 mL |
| 5 mM | 0.6796 mL | 3.3978 mL | 6.7956 mL | 16.9889 mL | |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3978 mL | 8.4944 mL | |
| 15 mM | 0.2265 mL | 1.1326 mL | 2.2652 mL | 5.6630 mL | |
| 20 mM | 0.1699 mL | 0.8494 mL | 1.6989 mL | 4.2472 mL | |
| 25 mM | 0.1359 mL | 0.6796 mL | 1.3591 mL | 3.3978 mL | |
| 30 mM | 0.1133 mL | 0.5663 mL | 1.1326 mL | 2.8315 mL | |
| 40 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1236 mL | |
| 50 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6989 mL | |
| 60 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4157 mL | |
| 80 mM | 0.0425 mL | 0.2124 mL | 0.4247 mL | 1.0618 mL | |
| 100 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL |
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