| Bioactivity | TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities[1]. | ||||||||||||
| Target | TAZ | ||||||||||||
| Invitro | 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: | ||||||||||||
| 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: | ||||||||||||
| Name | TM-25659 | ||||||||||||
| CAS | 260553-97-7 | ||||||||||||
| Formula | C30H28N8 | ||||||||||||
| Molar Mass | 500.60 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |