TM-25659
Based on 1 Customer Validation
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
For research use only. We do not sell to patients.
- Purity: 98.15%
- CAS No.: 260553-97-7
- Formula: C30H28N8
- Molecular Weight:500.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
All YAP Isoforms
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Biological Activity
TAZ[1]
TM-25659 (2, 10, 20, 100 μM) enhances nuclear TAZ localization in a dose-dependent manner and attenuates PPARγ-mediated adipocyte differentiation by facilitating PPARγ suppression activity of TAZ[1].
TM-25659 (2, 10, 50 μM) enhances osteogenic gene expression and thereby increases osteoblast differentiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:3T3-L1 cells
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Concentration:2, 10, 20, 100 μM
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Incubation Time:6 days
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Result:Acted as a suppressor of PPARγ-dependent adipocyte differentiation[1].
TM-25659 has a favourable pharmacokinetic profile in rats. The plasma concentration of TM-25659 declines with an approximate t1/2 of 7 or 10 h following i.v or p.o. administration respectively. The systemic clearance (CL) is 0.21 L×h-1×kg-1 and the volume of distribution at steady-state (1.91 L×h-1×kg-1) is larger than the volume of total body fluids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL6 mice (4- to 6-week-old )[1]
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Dosage:50 mg/kg
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Administration:I.p., every other day for 2 weeks
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Result:Attenuated weight gain in these obese mice[1].
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Animal Model:Adult male Sprague-Dawley rats[1]
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Dosage:10 mg/kg
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Administration:I.v. (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)
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Result:Oral administration for 4 weeks moderately but significantly attenuated weight gain and partly restored BMD in the OVX rats[1].
Chemical Information
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CAS No. 260553-97-7
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Appearance Solid
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Molecular Weight 500.60
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Formula C30H28N8
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Color White to off-white
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SMILES
CC1=C(C2=CC=CN=C2)C=C3C(N(CC4=CC=C(C5=CC=CC=C5C6=NN=NN6)C=C4)C(CCCC)=N3)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 135 mg/mL (269.68 mM; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.25 mg/mL (4.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: 2.25 mg/mL (4.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (604 KB)
- English - EN (604 KB)
- Français - FR (604 KB)
- Deutsch - DE (604 KB)
- Norwegian - NO (604 KB)
- Español - ES (604 KB)
- Swedish - SV (604 KB)
- Italian - IT (604 KB)
- Korean - KR (604 KB)
- Portuguese - PT (604 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9976 mL | 9.9880 mL | 19.9760 mL | 49.9401 mL |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9952 mL | 9.9880 mL | |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 mL | 4.9940 mL | |
| 15 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 20 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4970 mL | |
| 25 mM | 0.0799 mL | 0.3995 mL | 0.7990 mL | 1.9976 mL | |
| 30 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6647 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3995 mL | 0.9988 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4994 mL |