GR 159897
Based on 1 Customer Validation
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
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- Pureza: 99.6%
- No. CAS: 158848-32-9
- Fòrmula: C23H27FN2O2S
- Peso molecular:414.54
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
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NK2R 10 (pKi, Rat colon membrane) |
hNK2 9.51 (pKi, CHO cell) |
GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells[2].
GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM and 4T1 cells) treatment increases phosphorylation of P38, while inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM and 4THM but not in 4T1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1, 4THM, 4TLM and 67NR cells
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Concentration:10 μM, 30 μM
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Incubation Time:72 hours
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Result:Inhibited proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells.
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Cell Line:4TBM, 4TLM, 4THM and 4T1 cells
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Concentration:10 μM, 30 μM
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Incubation Time:40 hours
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Result:Increased phosphorylation of P38.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea-pigs[1]
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Dosage:0.12 mg/kg
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Administration:Intravenous injection
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Result:Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
Chemical Information
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No. CAS 158848-32-9
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Appearance Solid
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Peso molecular 414.54
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Fòrmula C23H27FN2O2S
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Color White to light yellow
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SMILES
O=[S@](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 31 mg/mL (74.78 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8. [Content Brief]
[2]. Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270. [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 (sealed storage, away from moisture). 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 | 2.4123 mL | 12.0616 mL | 24.1231 mL | 60.3078 mL |
| 5 mM | 0.4825 mL | 2.4123 mL | 4.8246 mL | 12.0616 mL | |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4123 mL | 6.0308 mL | |
| 15 mM | 0.1608 mL | 0.8041 mL | 1.6082 mL | 4.0205 mL | |
| 20 mM | 0.1206 mL | 0.6031 mL | 1.2062 mL | 3.0154 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9649 mL | 2.4123 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8041 mL | 2.0103 mL | |
| 40 mM | 0.0603 mL | 0.3015 mL | 0.6031 mL | 1.5077 mL | |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 60 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0051 mL |
GR 159897 Related Classifications
HY-107691 Related Classifications
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