TM-25659-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETM-25659Cat. No.: HY-112920CAS No.: 260553-97-7分式: CHN分量: 500.6作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 135 mg/mL (269.68 mM)H2O : 40% PEG300 5% Tween-80 45% sa

2、lineSolubility: 2.25 mg/mL (4.49 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (4.49 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (4.49 mM); Clear soluti

3、onBIOLOGICAL ACTIVITY物活性 TM-25659具有PDZ结合 序的转录共激活 (TAZ) 的调制剂。抗质疏松和抗肥胖活性 1。IC50 & Target TAZ 1体外研究 TM-25659 (2, 10, 20, 100 M) enhances nuclear TAZ localization in a dose-dependent manner andattenuates PPAR-mediated adipocyte differentiation by facilitating PPAR suppression activity of TAZ 1.TM-25659

4、(2, 10, 50 M) enhances osteogenic gene expression and thereby increases osteoblastdifferentiation 1.Cell Proliferation Assay 1Cell Line: 3T3-L1 cellsConcentration: 2, 10, 20, 100 MIncubation Time: 6 daysResult: Acted as a suppressor of PPAR-dependent adipocyte differentiation 1.体内研究TM-25659 (50 mg/k

5、g, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weightgain in an obesity model 1.TM-25659 has a favourable pharmacokinetic profile in rats. The plasma concentration of TM-25659 declineswith an approximate t1/2 of 7 or 10 h following i.v or p.o. administration respect

6、ively. The systemic clearance(CL) is 0.21 Lh-1kg-1 and the volume of distribution at steady-state (1.91 Lh-1kg-1) is larger than thevolume of total body fluids 1.Animal Model: C57BL6 mice (4- to 6-week-old ) 1Dosage: 50 mg/kgAdministration: I.p., every other day for 2 weeksResult: Attenuated weight

7、gain in these obese mice 1.Animal Model: Adult male Sprague-Dawley rats 1Dosage: 10 mg/kgAdministration: I.v. (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEResult: Oral administration for 4 weeks moderately but significantly attenuated

8、weight gain andpartly restored BMD in the OVX rats 1.REFERENCES1. Jang EJ, et al. TM-25659 enhances osteogenic differentiation and suppresses adipogenic differentiation by modulating thetranscriptional co-activator TAZ. Br J Pharmacol. 2012 Mar;165(5):1584-94.McePdfHeightCaution: Product has not been fully validated for medical applications.F