BAY 36-7620
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.9%
- CAS. Nr.: 232605-26-4
- Formel: C19H18O2
- Molecular Weight:278.35
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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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) |
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.
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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.
In Vivo
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.
- Kinase activity and phosphorylation assays
- Western Blot
- How to Select a Suitable Non-Mouse Animal Model
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
- How to Choose the Right Model Animal
Chemical Information
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CAS. Nr. 232605-26-4
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Appearance Solid
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Molecular Weight 278.35
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Formel C19H18O2
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Color White to yellow
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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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 42 mg/mL (150.89 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5926 mL | 17.9630 mL | 35.9260 mL | 89.8150 mL |
| 5 mM | 0.7185 mL | 3.5926 mL | 7.1852 mL | 17.9630 mL | |
| 10 mM | 0.3593 mL | 1.7963 mL | 3.5926 mL | 8.9815 mL | |
| 15 mM | 0.2395 mL | 1.1975 mL | 2.3951 mL | 5.9877 mL | |
| 20 mM | 0.1796 mL | 0.8981 mL | 1.7963 mL | 4.4907 mL | |
| 25 mM | 0.1437 mL | 0.7185 mL | 1.4370 mL | 3.5926 mL | |
| 30 mM | 0.1198 mL | 0.5988 mL | 1.1975 mL | 2.9938 mL | |
| 40 mM | 0.0898 mL | 0.4491 mL | 0.8981 mL | 2.2454 mL | |
| 50 mM | 0.0719 mL | 0.3593 mL | 0.7185 mL | 1.7963 mL | |
| 60 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4969 mL | |
| 80 mM | 0.0449 mL | 0.2245 mL | 0.4491 mL | 1.1227 mL | |
| 100 mM | 0.0359 mL | 0.1796 mL | 0.3593 mL | 0.8981 mL |
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