1256341-22-6

CX08005 is a competitive PTP1B inhibitor (IC50 = 0.781 μM). Binds catalytic P-loop of enzyme. Improves insulin sensitivity in obese mice in the glucose tolerance test and the homeostasis model assessment of insulin resistance index (HOMA-IR). Enhances insulin-induced glucose uptake in adipocytes and myotubes in vitro. Exhibits some selectivity for PTP1B over other protein tyrosine phosphatases, except TCPTP.

CX08005 is a cell-permeable benzoic acid based compoundpotent and substrate-competitive PTP1B/TCPTP dual inhibitor with anti-diabetic efficacy both in vitro and in vivo. CX08005 targets protein tyrosine phosphatase 1B (PTP1B) catalytic P-loop and acts as a substrate-competitive inhibitor against PTP1B and TCPTP (IC50 = 781 and 475 nMrespectively) with much reduced potency toward LARSHP1and VHR (by 52%89%and 60%respectively at 10 μM). CX08005 enhances insulin-dependent cellular signaling (Eff. conc. 10 nM; HepG2 cells) and glucose uptake (Eff. conc. 100-500 nM; 3T3-L1 adipocityes and C2C12 myoblasts) in vitroas well as improves glucose tolerance and insulin sensitivity in diet-induced obesity (DIO) mice and KKAy type 2 diabetes mice (50-200 mg/kg/day i.p.) in vivo with good pharmacokinetics in SD rats (Cmax = 7425.9 ng/mLTmax = 6.67 h,  t1/2

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