TM-25659

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.