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编 号：F285470
分子式：C19H18O2
分子量：278.35
分子式：C19H18O2
分子量：278.35
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CAS No: 232605-26-4
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生物活性：
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.
体内研究：
BAY 36-7620 (5-10 mg/kg，腹腔注射；每日 1 次，连续 24 天) 抑制了胸腺裸鼠模型的肿瘤生长，延长了肺癌肿瘤小鼠的寿命。BAY 36-7620 (0.01-0.03 mg/kg，静脉注射；4 小时) 对急性硬膜下血肿大鼠模型具有神经保护作用。Animal Model:Lung tumors mice model
Dosage:5, 10 mg/kg
Administration:Intraperitoneal injection (i.p.); Once daily for 24 days
Result:Suppressed tumor growth in athymic mice with lung tumors. Prolonged the survival of inoculated mice when compared to control group. Decreased the level of AKT phosphorylation in A549 tumors.
Animal Model:Subdural hematoma rat model
Dosage:0-3 mg/kg
Administration:Intravenous injection (i.v.); 4 h
Result:Had neuroprotective effect with the efficacy of 40–50% at 0.01 and 0.03 mg/kg.
体外研究：
BAY 36-7620 (0.1-10 μM) 在浓度 10 μM 时完全抑制了 HEK 293 细胞中的 mGlu1 受体BAY 36-7620 相关抗体:Western Blot AnalysisCell Line:A549 cell line
Concentration:10, 25 μM
Incubation Time:Overnight
Result:Enhanced the expression of cleaved PARP and reduced bcl-2 protein expression. Reduced the expression of HIF-1α protein and HIF activity. Reduced the secretion of VEGF and IL-8 into supernatants.
Cell Proliferation AssayCell Line:T MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T and BT-549 cell line
Concentration:50 μM
Incubation Time:72 h
Result:Decreased the percentage of proliferating cells in all breast cancercell line.
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.
体内研究：
BAY 36-7620 (5-10 mg/kg，腹腔注射；每日 1 次，连续 24 天) 抑制了胸腺裸鼠模型的肿瘤生长，延长了肺癌肿瘤小鼠的寿命。BAY 36-7620 (0.01-0.03 mg/kg，静脉注射；4 小时) 对急性硬膜下血肿大鼠模型具有神经保护作用。Animal Model:Lung tumors mice model
Dosage:5, 10 mg/kg
Administration:Intraperitoneal injection (i.p.); Once daily for 24 days
Result:Suppressed tumor growth in athymic mice with lung tumors. Prolonged the survival of inoculated mice when compared to control group. Decreased the level of AKT phosphorylation in A549 tumors.
Animal Model:Subdural hematoma rat model
Dosage:0-3 mg/kg
Administration:Intravenous injection (i.v.); 4 h
Result:Had neuroprotective effect with the efficacy of 40–50% at 0.01 and 0.03 mg/kg.
体外研究：
BAY 36-7620 (0.1-10 μM) 在浓度 10 μM 时完全抑制了 HEK 293 细胞中的 mGlu1 受体BAY 36-7620 相关抗体:Western Blot AnalysisCell Line:A549 cell line
Concentration:10, 25 μM
Incubation Time:Overnight
Result:Enhanced the expression of cleaved PARP and reduced bcl-2 protein expression. Reduced the expression of HIF-1α protein and HIF activity. Reduced the secretion of VEGF and IL-8 into supernatants.
Cell Proliferation AssayCell Line:T MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T and BT-549 cell line
Concentration:50 μM
Incubation Time:72 h
Result:Decreased the percentage of proliferating cells in all breast cancercell line.
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