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.
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- CAS. Nr.: 232605-26-4
- Formel: C19H18O2
- Molecular Weight:278.35
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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mGluR 1 0.16 μM (IC50) |
mGluR1a 0.38 μM (IC50) |
mGluR2 0.14 μM (IC50) |
mGluR 5 0.24 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cell line
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Concentration:10, 25 μM
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Incubation Time:Overnight
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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.
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Cell Line:T MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T and BT-549 cell line
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Concentration:50 μM
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Incubation Time:72 h
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Result:Decreased the percentage of proliferating cells in all breast cancer cell line.
BAY 36-7620 (0.01-0.03 mg/kg for i.v.; 4 h) has neuroprotective effect in acute subdural hematoma rat model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lung tumors mice model[2]
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Dosage:5, 10 mg/kg
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Administration:Intraperitoneal injection (i.p.); Once daily for 24 days
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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.
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Animal Model:Subdural hematoma rat model[4]
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Dosage:0-3 mg/kg
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Administration:Intravenous injection (i.v.); 4 h
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Result:Had neuroprotective effect with the efficacy of 40–50% at 0.01 and 0.03 mg/kg.
Chemical Information
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CAS. Nr. 232605-26-4
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Molecular Weight 278.35
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Formel C19H18O2
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SMILES
C=C(C1)C[C@@](COC2=O)([H])[C@@]12CC3=CC4=C(C=CC=C4)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Carroll FY, et al. BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol Pharmacol. 2001 May;59(5):965-73. [Content Brief]
[2]. Xia H, et al. Inhibition of metabotropic glutamate receptor 1 suppresses tumor growth and angiogenesis in experimental non-small cell lung cancer. Eur J Pharmacol. 2016 Jul 15;783:103-11. [Content Brief]
[3]. Dolfi SC, et al. Riluzole exerts distinct antitumor effects from a metabotropic glutamate receptor 1-specific inhibitor on breast cancer cells. Oncotarget. 2017 Jul 4;8(27):44639-44653. [Content Brief]
[4]. De Vry J, et al. Neuroprotective and behavioral effects of the selective metabotropic glutamate mGlu(1) receptor antagonist BAY 36-7620. Eur J Pharmacol. 2001 Oct 5;428(2):203-14. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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