CX-08005

CX-08005 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC₅₀ = 0.781 µM).¹ It is selective for PTP1B over Src homology region 2 domain-containing phosphatase 1 (SHP-1), dual-specificity phosphatase 3 (DUSP3), and leukocyte common antigen-related (LAR) phosphatase at 10 µM but does inhibit T cell protein tyrosine phosphatase (TCPTP; IC₅₀ = 0.475 µM). CX-08005 (100 and 200 mg/kg) decreases blood glucose levels in a glucose tolerance test in a mouse model of high-fat diet-induced obesity (DIO). It also increases red blood cell velocity and central and interlobular veins shear rates and decreases rolling and adhering leukocyte numbers in a mouse model of DIO when administered at a dose of 100 mg/kg.² CX-08005 (50 mg/kg) decreases hepatic and plasma triglyceride levels in a KKAy mouse model of diabetes.

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1. Zhang, X., Tian, J., Li, J., et al. A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance. Br. J. Pharmacol. 173(12), 1939-1949 (2016).

2. Li, J., Zhang, X., Tian, J., et al. CX08005, a protein tyrosine phosphatase 1B inhibitor, attenuated hepatic lipid accumulation and microcirculation dysfunction associated with nonalcoholic fatty liver disease. Pharmaceuticals (Basel) 16(1), 106 (2023).