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TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.

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TM-25659 Chemical Structure

TM-25659 Chemical Structure

CAS No. : 260553-97-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

TM-25659 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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Description

TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities[1].

IC50 & Target

TAZ[1]
In Vitro

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.

TM-25659 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: 3T3-L1 cells
Concentration: 2, 10, 20, 100 μM
Incubation Time: 6 days
Result: Acted as a suppressor of PPARγ-dependent adipocyte differentiation[1].
In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 mice (4- to 6-week-old )[1]
Dosage: 50 mg/kg
Administration: I.p., every other day for 2 weeks
Result: Attenuated weight gain in these obese mice[1].
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: Oral administration for 4 weeks moderately but significantly attenuated weight gain and partly restored BMD in the OVX rats[1].
Molecular Weight

500.60

Formula

C30H28N8
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9976 mL 9.9880 mL 19.9760 mL
5 mM 0.3995 mL 1.9976 mL 3.9952 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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TM-25659 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TM-25659260553-97-7TM25659TM 25659OthersInhibitorinhibitorinhibit

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