TM-25659 |
| カタログ番号GC33782 |
TM-25659 は、PDZ 結合モチーフ (TAZ) モジュレーターを持つ転写コアクチベーターです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 260553-97-7
Sample solution is provided at 25 µL, 10mM.
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TM-25659 is a TAZ modulator. Anti-osteoporotic and anti-obesity activities[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].|| Cell Proliferation Assay[1]||Cell Line:|3T3-L1 cells|Concentration:|2, 10, 20, 100 μM|Incubation Time:|6 days|Result:|TM-25659 acted as a suppressor of PPARγ-dependent adipocyte differentiation[1].
TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weight gain in an obesity model[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].|| Animal Model:|C57BL6 mice (4- to 6-week-old )[1]|Dosage:|50 mg/kg|Administration:|i.p., every other day for 2 weeks|Result:||| Animal Model:|Adult male Sprague-Dawley rats[1]|Dosage:|10 mg/kg|Administration:|i.v (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)|Result:|
[1]. Jang EJ, et al. TM-25659 enhances osteogenic differentiation and suppresses adipogenic differentiation by modulating the transcriptional co-activator TAZ. Br J Pharmacol. 2012 Mar;165(5):1584-94.
| Cas No. | 260553-97-7 | SDF | |
| Canonical 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 | ||
| Formula | C30H28N8 | M.Wt | 500.6 |
| 溶解度 | DMSO : ≥ 135 mg/mL (269.68 mM);Water : < 0.1 mg/mL (insoluble) | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9976 mL | 9.988 mL | 19.976 mL |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9952 mL |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 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 ddH2O, 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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