您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > BR102375
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
BR102375
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BR102375图片
CAS NO:2366255-59-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BR102375 是一种用于治疗 2 型糖尿病的 non-TZD (噻唑烷二酮类) PPAR γ 完全激动剂, 其 EC50 值和 Amax比率值分别为 0.28 μM 和 98%。
Cas No.2366255-59-4
Canonical SMILESCCCCC(N1CC2=CC=C(C3=C(C4=NOC(N4)=O)C=CC=C3)C=C2)=NC(C)=C(CC5=NC(C(C)(C)C)=NO5)C1=O
分子式C31H34N6O4
分子量554.64
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%[1].

BR102375 (Compound 18) (10 μM) increases gene expression levels relevant to PPARγ activation and enhances glucose uptake under insulin stimulation[1].BR102375 (Compound 18) (10 nM, 100 nM, 1 μM; 6 days, 14 days) shows a concentration-dependent, insulin-sensitive effects on adipogenesis[1]. RT-PCR[1] Cell Line: 3T3-L1 mouse preadipocyte cells

BR102375 (Compound 18) has decent efficacy on mouse diabetes model[1].BR102375 reveals significant suppressive effect on random blood glucose increase(75 mpk, p.o., bid), shows decent effect on insulin resistance on Oral glucose tolerance test (OGTT) and discloses similar findings in body weight gain almost identical to Pioglitazone[1].

[1]. Choung W, et al. Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2019 Jun 19. pii: S0960-894X(19)30407-X.