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说明： High affinity NK1 antagonist
化学名： (4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
纯度： ≥98% (HPLC)
生物活性 for FK 888
FK 888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. Inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo following i.v. and oral administration.
许可信息
Sold with the permission of Astellas Pharma Inc.
技术数据 for FK 888
| 分子量 | 588.69 |
| 公式 | C36H36N4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 138449-07-7 |
| PubChem ID | 107967 |
| InChI Key | BFNKQTIJVFGCKQ-PDJGWCFMSA-N |
| Smiles | O=C(N3[C@H]([C@](N[C@@H](CC5=CC(C=CC=C6)=C6C=C5)C(N(C)CC4=CC=CC=C4)=O)=O)C[C@@H](O)C3)C2=CN(C)C1=CC=CC=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for FK 888
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 58.87 | 100 | |
| ethanol | 58.87 | 100 |
制备储备液 for FK 888
以下数据基于产品分子量 588.69。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.7 mL | 8.49 mL | 16.99 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.4 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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产品说明书 for FK 888
参考文献 for FK 888
参考文献是支持产品生物活性的出版物。
Fujii et al (1992) Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist. Br.J.Pharmacol. 107 785 PMID: 1282073
Murai et al (1993) Effects of an NK1 receptor antagonist, FK888, on constriction and plasma extravasation induced in guinea pig airway by neurokinins and capsaicin. Eur.J.Pharmacol. 236 7 PMID: 7686493
Aramori et al (1994) Subtype- and species-selectivity of a tachykinin receptor antagonist, FK888, for cloned rat and human tachykinin receptors. Eur.J.Pharmacol. 269 277 PMID: 7531648
If you know of a relevant reference for FK 888, please let us know.
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关键词: FK 888, FK 888 supplier, High, affinity, NK1, receptor, antagonists, Tachykinin, Receptors, Neurokinin, FK888, Receptor, 2400, Tocris Bioscience
1 篇 FK 888 的引用文献
引用文献是使用了 Tocris 产品的出版物。 FK 888 的部分引用包括：
Mondal et al (2013) Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons. PLoS One 8 e60365 PMID: 23565235
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