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TM-25659 

Cat. No.: HY-112920 Purity: 99.16%
Handling Instructions

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.

TM-25659 Chemical Structure

TM-25659 Chemical Structure

CAS No. : 260553-97-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

260553-97-7

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 135 mg/mL (269.68 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.1998 mL 0.9988 mL 1.9976 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (4.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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TM-25659
Cat. No.:
HY-112920
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