TK-129 |
Catalog No.GC70033
One-Click Copy Product Info
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TK-129 est un inhibiteur puissant et à faible toxicité de KDM5B par voie orale (avec une forte affinité ; IC50=44 nM). TK-129 exerce une action protectrice sur le cœur en inhibant KDM5B et en bloquant la voie Wnt associée à KDM5B. En vitro, TK-129 réduit l'activation des fibroblastes cardiaques induite par Ang II, tandis qu'en vivo il réduit la remodélisation et la fibrose myocardiques induites par l'adrénaline isopropylique. TK-129 peut être utilisé dans la recherche sur les maladies cardiovasculaires.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3031476-73-7
Sample solution is provided at 25 µL, 10mM.
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TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease[1].
References:
[1]. Tang K, et al. Discovery of Novel Pyrazole-Based KDM5B Inhibitor TK-129 and Its Protective Effects on Myocardial Remodeling and Fibrosis. J Med Chem. 2022 Sep 16.
| Cas No. | 3031476-73-7 | SDF | |
| Formula | C15H23N5O2 | M.Wt | 305.38 |
| Solubility | DMSO : 100 mg/mL (327.46 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2746 mL | 16.373 mL | 32.7461 mL |
| 5 mM | 654.9 μL | 3.2746 mL | 6.5492 mL |
| 10 mM | 327.5 μL | 1.6373 mL | 3.2746 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)