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260553-97-7

中文名稱 TM-25659
英文名稱 TM-25659
CAS 260553-97-7
分子式 C30H28N8
分子量 500.6
MOL 文件 260553-97-7.mol
更新日期 2023/03/20 15:41:25
260553-97-7 結(jié)構(gòu)式 260553-97-7 結(jié)構(gòu)式

基本信息

中文別名
3-((2'-(2H-四唑-5-基)-[1,1'-聯(lián)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
英文別名
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]-

物理化學(xué)性質(zhì)

沸點768.0±70.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : ≥ 135 mg/mL (269.68 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)4.15±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
TM-25659價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-112920TM-25659
TM-25659
260553-97-75mg950元
2024/11/08HY-112920TM-25659
TM-25659
260553-97-710mM * 1mLin DMSO1050元
2024/11/08HY-112920TM-25659
TM-25659
260553-97-710mg1500元

常見問題列表

生物活性
TM-25659是 具有PDZ結(jié)合基序的轉(zhuǎn)錄共激活子 (TAZ) 的調(diào)制劑。抗骨質(zhì)疏松和抗肥胖活性。
靶點

TAZ

體外研究

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] .
體內(nèi)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] .
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