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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.6%
- CAS 番号: 158848-32-9
- 分子式: C23H27FN2O2S
- 分子量:414.54
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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).
化学情報
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CAS 番号 158848-32-9
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性状 Solid
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分子量 414.54
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-107691 関連分類
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