ATX inhibitor 5
Based on 1 Customer Validation
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.
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- Pureté : 98.71%
- CAS No.: 2402772-45-4
- Formule: C22H18ClF3N6O
- Masse moléculaire:474.87
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
Autotaxin |
In Vitro
ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC)[1].
ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:CFs and t-HSC/Cl-6 cells
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Concentration:0.0001, 0.01, 1, 100, 10000 µM
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Incubation Time:48 hours
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Result:Displayed activities against CFs and t-HSC/Cl-6 cells with IC50s of 1.21 and 0.78 µM, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Konmin mice (8-week old, 22-25 g)[1]
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Dosage:20, 40 mg/kg
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Administration:Orally; once daily for two weeks
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Result:Prominently reduced CCl4-induced hepatic fibrosis level.
Chemical Information
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CAS No. 2402772-45-4
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Appearance Solid
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Masse moléculaire 474.87
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Formule C22H18ClF3N6O
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Color White to off-white
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SMILES
O=C(N/N=C/C1=CC=C(Cl)C=C1)N(C2)CCC3=C2C(NC4=CC=CC(C(F)(F)F)=C4)=NC=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (526.46 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: ≥ 2.08 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Protocole
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
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- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.1058 mL | 10.5292 mL | 21.0584 mL | 52.6460 mL |
| 5 mM | 0.4212 mL | 2.1058 mL | 4.2117 mL | 10.5292 mL | |
| 10 mM | 0.2106 mL | 1.0529 mL | 2.1058 mL | 5.2646 mL | |
| 15 mM | 0.1404 mL | 0.7019 mL | 1.4039 mL | 3.5097 mL | |
| 20 mM | 0.1053 mL | 0.5265 mL | 1.0529 mL | 2.6323 mL | |
| 25 mM | 0.0842 mL | 0.4212 mL | 0.8423 mL | 2.1058 mL | |
| 30 mM | 0.0702 mL | 0.3510 mL | 0.7019 mL | 1.7549 mL | |
| 40 mM | 0.0526 mL | 0.2632 mL | 0.5265 mL | 1.3161 mL | |
| 50 mM | 0.0421 mL | 0.2106 mL | 0.4212 mL | 1.0529 mL | |
| 60 mM | 0.0351 mL | 0.1755 mL | 0.3510 mL | 0.8774 mL | |
| 80 mM | 0.0263 mL | 0.1316 mL | 0.2632 mL | 0.6581 mL | |
| 100 mM | 0.0211 mL | 0.1053 mL | 0.2106 mL | 0.5265 mL |
ATX inhibitor 5 Related Classifications
HY-133019 Related Classifications
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