TM-25659是 具有PDZ结合基序的转录共激活子 (TAZ) 的调制剂。抗骨质疏松和抗肥胖活性。

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

Solid

TAZ

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.TM-25659 (2, 10, 50 μM) enhances osteogenic gene expression and thereby increases osteoblast differentiation. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

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. TM-25659 has a favourable pharmacokinetic profile in rats. The plasma concentration of TM-25659 declines with an approximate t 1/2 of 7 or 10 h following i.v or p.o. administration respectively. The systemic clearance (CL) is 0.21 L×h×kg and the volume of distribution at steady-state (1.91 L×h×kg) is larger than the volume of total body fluids. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 135 mg/mL (269.68 mM)配制储备液