TM-25659

生物活性靶点体外研究体内研究 TM-25659 试剂级价格

TM-25659

CAS号:260553-97-7
英文名:TM-25659
中文名:TM-25659
CBNumber:CB84845065
分子式:C30H28N8
分子量:500.6
MOL File:260553-97-7.mol

TM-25659化学性质

沸点 :768.0±70.0 °C(Predicted)
密度 :1.29±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO : ≥ 135 mg/mL (269.68 mM);Water : < 0.1 mg/mL (insoluble)
形态 :Solid
酸度系数(pKa) :4.15±0.10(Predicted)
颜色 :White to off-white

TM-25659性质、用途与生产工艺

生物活性 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。
靶点

TAZ

体外研究

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.

Cell Proliferation Assay

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] .

体内研究

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 ^-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.

Animal Model:	C57BL6 mice (4- to 6-week-old )
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
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] .