BAY 36-7620

BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC₅₀=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research^[1][2][3][4]. IC50 & Target:IC50: 0.16 μM (mGlu1), 0.38 μM (mGlu1a), 0.14 μM (mGlu2/1), 0.24 μM (mGlu5), 0.50 μM (mGlu5/1-F)^[1] In Vitro:BAY 36-7620 (0.1-10 μM) completely inhibits mGlu1 receptors 10 μM in HEK 293 Cells^[1].
BAY 36-7620 (10-25 μM, 4 days) reduces cell proliferation and inhibits tumor-related protein expression in A549 cells^[2].
BAY 36-7620 (72 h) inhibits MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T and BT-549 cell growth and proliferation with IC₅₀s of 27.7, 37.1, 20.8, 41.0, 21.0 and 15.7μM, respectively^[3].
BAY 36-7620 (25-50 μM, 24-72 h) causes DNA damage and induces modest G2/M arrest in T-47D, BT-474, MDA-MB-231, and BT-549 cell lines^[3]. In Vivo:BAY 36-7620 (5-10 mg/kg for i.p; once daily for 24 days) inhibits tumor growth and prolongs the survival of Lung tumors mice model ^[2].
BAY 36-7620 (0.01-0.03 mg/kg for i.v.; 4 h) has neuroprotective effect in acute subdural hematoma rat model^[4].