1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. 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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BAY 36-7620 Chemical Structure

BAY 36-7620 Chemical Structure

CAS No. : 232605-26-4

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Description

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

mGluR 1

0.16 μM (IC50)

mGluR1a

0.38 μM (IC50)

mGluR2

0.14 μM (IC50)

mGluR 5

0.24 μM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell 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 Assay[3]

Cell 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 cancer cell line.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lung tumors mice model[2]
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[4]
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.
Molecular Weight

278.35

Formula

C19H18O2

CAS No.
SMILES

C=C(C1)C[C@@](COC2=O)([H])[C@@]12CC3=CC4=C(C=CC=C4)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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BAY 36-7620 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BAY 36-7620
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