TK-112690
Based on 1 Customer Validation
TK-112690 is a UPP1 inhibitor. TK-112690 inhibits murine small intestinal uridine phosphorylase (UPase) with an IC50 of 12.5 μM and human small intestinal UPase with an IC50 of 20.0 μM in vitro. TK-112690 increases plasma uridine concentration in mice. TK-112690 can be used for the study of cancer and pulmonary fibrosis.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 22423-26-3
- Formula: C10H12N2O5
- Molecular Weight:240.21
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vivo
TK-112690 (60 mg/kg, i.p., 3 h before and after MTX on Days 2-4, 7 days) reduces MTX-induced mucosal permeability loss in C57BL/6 female mice[2].
TK-112690 (120 mg/kg, i.p., detected at 0.08-12 h post-dose) increases plasma uridine concentration in CD-1 female mice[2].
TK-112690 (667-3000 mg/kg/day, continuous s.c. infusion via osmotic pumps for 24-72 h) elevates plasma uridine (UR) concentration in a linear manner in BDF-1 mice[3].
TK-112690 (60 mg/kg, i.p., twice daily with 6-8 h interval on Days 7-20) reduces pulmonary fibrosis in C57BL/6 mice with Bleomycin (HY-108345)-induced fibrosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 mice[2]
-
Dosage:10, 30 mg/kg
-
Administration:i.p., 3 h before and after methotrexate (HY-14519) on Days 2-3, 4 weeks
-
Result:Mitigated MTX-induced weight loss in LPS-treated C57BL/6 mice.
-
Animal Model:C57BL/6 mice[2]
-
Dosage:120 mg/kg
-
Administration:i.p., detected at 0.08-12 h post-dose
-
Result:Reduced MTX-induced mucosal permeability loss in C57BL/6 female mice.
-
Animal Model:CD-1 female mice[2]
-
Dosage:120 mg/kg
-
Administration:i.p., detected at 0.08-12 h post-dose
-
Result:Increased plasma uridine concentration in CD-1 female mice.
-
Animal Model:BDF-1 mice[3]
-
Dosage:667, 833, 3000 mg/kg/day
-
Administration:s.c. infusion via osmotic pumps for 24-72 h
-
Result:Elevated plasma uridine (UR) concentration in a linear manner in BDF-1 mice.
-
Animal Model:C57BL/6 mice[3]
-
Dosage:60 mg/kg
-
Administration:i.p., twice daily with 6-8 h interval on Days 7-20
-
Result:Reduced pulmonary fibrosis in C57BL/6 mice with Bleomycin (HY-108345)-induced fibrosis.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 22423-26-3
-
Appearance Solid
-
Molecular Weight 240.21
-
Formula C10H12N2O5
-
Color White to off-white
-
SMILES
CC(C1=O)=CN(C2=N1)[C@@]3([H])[C@](O2)([H])[C@@](O)([H])[C@@](O3)([H])CO
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
H2O : ≥ 100 mg/mL (416.30 mM)
DMSO : 50 mg/mL (208.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 5 mg/mL (20.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (20.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocols
-
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
-
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.
-
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.
-
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
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
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 / H2O | 1 mM | 4.1630 mL | 20.8151 mL | 41.6302 mL | 104.0756 mL |
| 5 mM | 0.8326 mL | 4.1630 mL | 8.3260 mL | 20.8151 mL | |
| 10 mM | 0.4163 mL | 2.0815 mL | 4.1630 mL | 10.4076 mL | |
| 15 mM | 0.2775 mL | 1.3877 mL | 2.7753 mL | 6.9384 mL | |
| 20 mM | 0.2082 mL | 1.0408 mL | 2.0815 mL | 5.2038 mL | |
| 25 mM | 0.1665 mL | 0.8326 mL | 1.6652 mL | 4.1630 mL | |
| 30 mM | 0.1388 mL | 0.6938 mL | 1.3877 mL | 3.4692 mL | |
| 40 mM | 0.1041 mL | 0.5204 mL | 1.0408 mL | 2.6019 mL | |
| 50 mM | 0.0833 mL | 0.4163 mL | 0.8326 mL | 2.0815 mL | |
| 60 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7346 mL | |
| 80 mM | 0.0520 mL | 0.2602 mL | 0.5204 mL | 1.3009 mL | |
| 100 mM | 0.0416 mL | 0.2082 mL | 0.4163 mL | 1.0408 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
TK-112690 Related Classifications
HY-W008491 Related Classifications
Powered by Bioz