IMM-H007

IMM-H007 is an activator of AMP-activated protein kinase (AMPK) and an antagonist of TGF-beta1. It increases AMPK activity in HepG2 cell lysates when used at concentrations ranging from 1 to 100 µM. IMM-H007 binds to TGF-beta1 (Kd = 0.2098 µM) and inhibits the binding of TGF-beta1 to TGF-beta receptor type 2 (TGFBR2) when used at a concentration of 6 µM. 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. 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. IMM-H007 (200 mg/kg) decreases fibrotic area in wild-type and AMPKalpha2 knockout mice in a model of cardiac fibrosis induced by the beta-adrenergic receptor (beta-AR) agonist isoprenaline (isoproterenol, Cay-15592). It decreases atherosclerotic lesion area in ApoE-/- mice fed a Paigen diet.Formal Name: N-(3-hydroxyphenyl)-adenosine 2',3',5'-triacetate. CAS Number: 1221412-23-2. Molecular Formula: C22H23N5O8. Formula Weight: 485.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=C(C)O[C@H]1[C@H](N2C3=NC=NC(NC4=CC=CC(O)=C4)=C3N=C2)O[C@H](COC(C)=O)[C@H]1OC(C)=O. InChi Code: InChI=1S/C22H23N5O8/c1-11(28)32-8-16-18(33-12(2)29)19(34-13(3)30)22(35-16)27-10-25-17-20(23-9-24-21(17)27)26-14-5-4-6-15(31)7-14/h4-7,9-10,16,18-19,22,31H,8H2,1-3H3,(H,23,24,26)/t16-,18-,19-,22-/m1/s1. InChi Key: IUDLPZTURGVXEA-WGQQHEPDSA-N.