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.