IMM-H007

IMM-H007 is an activator of AMP-activated protein kinase (AMPK) and an antagonist of TGF-β1.^1,2 It increases AMPK activity in HepG2 cell lysates when used at concentrations ranging from 1 to 100 µM.¹ IMM-H007 binds to TGF-β1 (K_d = 0.2098 µM) and inhibits the binding of TGF-β1 to TGF-β receptor type 2 (TGFBR2) when used at a concentration of 6 µM.² It increases cholesterol efflux in THP-1 macrophages incubated with isolated mouse ApoB-depleted serum ex vivo when administered at a dose of 100 or 200 mg/kg.³ In vivo, IMM-H007 (18 mg/kg) decreases serum levels of triglycerides, total cholesterol, and LDL cholesterol, as well as hepatic lipid accumulation, in a hamster model of high-fat diet-induced hyperlipidemia.¹ IMM-H007 (200 mg/kg) decreases fibrotic area in wild-type and AMPKα2 knockout mice in a model of cardiac fibrosis induced by the β-adrenergic receptor (β-AR) agonist isoprenaline (isoproterenol; Item No. 15592).² It decreases atherosclerotic lesion area in ApoE^-/- mice fed a Paigen diet.³

WARNING This product is not for human or veterinary use.

1. Lian, Z., Li, Y., Gao, J., et al. A novel AMPK activator, WS070117, improves lipid metabolism discords in hamsters and HepG2 cells. Lipids Health Dis. 10, 67 (2011).

2. Wang, S.-X., Feng, Y.-N., Feng, S., et al. IMM-H007 attenuates isoprenaline-induced cardiac fibrosis through targeting TGFβ1 signaling pathway. Acta Pharmacol. Sin. 43(10), 2542-2549 (2022).

3. Huang, L., Fan, B., Ma, A., et al. Inhibition of ABCA1 protein degradation promotes HDL cholesterol efflux capacity and RCT and reduces atherosclerosis in mice. J. Lipid Res. 56(5), 986-997 (2015).