Art. -Nr.: HY-139585

Tigulixostat

Name: Tigulixostat
Brand: MedChemExpress
SKU: HY-139585
Price: 300.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: LC350189)

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.18%
CAS. Nr.: 1287766-55-5
Formel: C₁₆H₁₄N₄O₂
Molecular Weight:294.31

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tigulixostat Chemical Structure

CAS. Nr.: 1287766-55-5

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Biologische Aktivität
- Beschreibung
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vivo

Tigulixostat (20 mg/kg; oral gavage; until 11 weeks of age) can effectively reduce serum uric acid levels, promote M2 macrophage polarization, and alleviate hyperuricemic nephropathy in urate oxidase knockout (Uox-KO) mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1287766-55-5
Appearance Solid
Molecular Weight 294.31
Formel C₁₆H₁₄N₄O₂
Color White to light yellow
SMILES

N#CC1=CN(C(C)C)C2=C1C=C(N3N=CC(C(O)=O)=C3)C=C2
Synonyms

LC350189
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3978 mL

16.9889 mL

33.9778 mL

5 mM

0.6796 mL

3.3978 mL

6.7956 mL

10 mM

0.3398 mL

1.6989 mL

3.3978 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[4]. Kumar A, et al. AB0101 PRECLINICAL IN VITRO AND IN VIVO EFFICACY STUDIES OF TIGULIXOSTAT, A SELECTIVE NON-PURINE XANTHINE OXIDASE INHIBITOR. Annals of the Rheumatic Diseases, 2024, 83: 1284.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Tigulixostat