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BAY 36-7620

CAS No. : 232605-26-4

MCE 国际站：BAY 36-7620

产品活性：BAY 36-7620 是有效的，非竞争性的并且有反向激动剂活性的 mGlu1 Receptor 的拮抗剂(IC₅₀ 为 0.16 μM)。BAY 36-7620 通过抑制 mGlu1 受体来抑制肿瘤生长并延长肿瘤小鼠寿命。BAY 36-7620 抑制 A549 肿瘤中的 AKT 磷酸化。BAY 36-7620 对急性硬膜下血肿大鼠模型具有神经保护作用。BAY 36-7620 可用于非小细胞肺癌和乳腺癌研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: BAY 36-7620 (0.1-10 μM) completely inhibits mGlu1 receptors 10 μM in HEK 293 Cells.
BAY 36-7620 (10-25 μM, 4 days) reduces cell proliferation and inhibits tumor-related protein expression in A549 cells.
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.
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.

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 .
BAY 36-7620 (0.01-0.03 mg/kg for i.v.; 4 h) has neuroprotective effect in acute subdural hematoma rat model.

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