TM-25659

TM-25659

中文名称TM-25659
中文同义词3-((2'-(2H-四唑-5-基)-[1,1'-联苯]-4-基)甲基)-2-丁基-5-甲基-6-(吡啶-3-基)-3H-咪唑并[4,5-B]吡啶;化合物 T13169;化合物TM-25659;3-((2'-(2H-四唑-5-基)-[1,1'-联苯]-4-基)甲基)-2-丁基-5-甲基-6-(吡啶-3-基)-3H-咪唑并[4,5-B]吡啶
英文名称TM-25659
英文同义词TM-25659;3H-Imidazo[4,5-b]pyridine, 2-butyl-5-methyl-6-(3-pyridinyl)-3-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-;TM 25659,TM25659;3-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-5-methyl-6-(pyridin-3-yl)-3H-imidazo[4,5-b]pyridine;3-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-5-methyl-6-(pyridin-3-yl)-3H-imidazo[4,5-b]pyridine
CAS号260553-97-7
分子式C30H28N8
分子量500.6
EINECS号
相关类别
Mol文件260553-97-7.mol
结构式TM-25659 结构式

TM-25659 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);水:< 0.1 mg/mL(不溶)
酸度系数(pKa)4.15±0.10(Predicted)

TM-25659 用途与合成方法

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。

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.

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] .

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] .

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-112920TM-25659
TM-25659
260553-97-75mg1600元
2024/01/25HY-112920TM-25659
TM-25659
260553-97-710mM * 1mLin DMSO1760元

TM-25659 上下游产品信息

"TM-25659"相关产品信息
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