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：2366255-59-4
分子式：C31H34N6O4
分子量：554.64
纯度：98%
存储：Store at -20°C

Background:

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.