TM-25659

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TM-25659 是一种具有 PDZ 结合基序 (TAZ) 的转录共激活因子调节剂，具有抗骨质疏松和抗肥胖活性。

TM-25659 is a modulator of transcriptional co-activator with PDZ-binding motif (TAZ), with anti-osteoporotic and anti-obesity activities.(In Vitro):Treatment with TM-25659 (2, 10, 20, 100 μM) dose-dependently enhances nuclear TAZ localization and attenuates PPARγ-mediated adipocyte differentiation by facilitating PPARγ suppression activity of TAZ. Osteogenic gene expression is enhanced by TM-25659 (2, 10, 50 μM) and thereby osteoblast differentiation is increased.(In Vivo):In vivo, TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss and decreases weight gain in an obesity model. 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×kg) and the volume of distribution at steady-state (1.91 L/(h×kg)) is larger than the volume of total body fluids.

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.

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.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.

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Others

Other Targets

HCV

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260553-97-7

500.6

C30H28N8

>98% (HPLC)

In Vitro:?DMSO : ≥ 135 mg/mL (269.68 mM)

CCCCc1nc2cc(-c3cccnc3)c(C)nc2n1Cc1ccc(cc1)-c1ccccc1-c1nn[nH]n1

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(-20℃)

With Ice Pack

≥ 2 years