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说明： Potent long-acting hNK1 antagonist
化学名： 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one
纯度： ≥99% (HPLC)
生物活性 for Aprepitant
Aprepitant is a potent long-acting hNK-1 antagonist (IC50 = 0.09 nM and Kd = 19 pM) that inhibits the effect of substance P on NK-1 receptors. Inhibits metastasis and impairs tumor growth in patient derived xenografts and breast cancer cells. In an animal model of intracerebral hemorrhage, Aprepitant reduces neurological impairment, neuronal damage and neuronal death. Suppresses pain and inflammation induced by formalin. Inhibits induced foot-tapping in gerbils. CNS penetrant and orally bioavailable. Antiemetic.
化合物库 for Aprepitant
Aprepitant is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Aprepitant
| 分子量 | 534.43 |
| 公式 | C23H21F7N4O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 170729-80-3 |
| PubChem ID | 6918365 |
| InChI Key | ATALOFNDEOCMKK-OITMNORJSA-N |
| Smiles | C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)O[C@H]2OCCN([C@H]2C3=CC=C(C=C3)F)CC4=NNC(N4)=O |
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 Aprepitant
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 53.44 | 100 | |
| ethanol | 5.34 | 10 |
制备储备液 for Aprepitant
以下数据基于产品分子量 534.43。 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 | 1.87 mL | 9.36 mL | 18.71 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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产品说明书 for Aprepitant
参考文献 for Aprepitant
参考文献是支持产品生物活性的出版物。
Hale et al (1998) Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 recepto J.Med.Chem. 41 4607 PMID: 9804700
Jin et al (2022) Aprepitant attenuates NLRC4-dependent neuronal pyroptosis via NK1R/PKCd pathway in a mouse model of intracerebral hemorrhage. J.Neuroinflammation 19 198 PMID: 35922848
Padmanaban et al (2024) Neuronal substance P drives metastasis through an extracellular RNA-TLR7 axis. Nature 633 207 PMID: 39112700
Yang et al (2022) Aprepitant inhibits JNK and p38/MAPK to attenuate inflammation and suppresses inflammatory pain. Front.Pharmacol. 12 811584 PMID: 35087409
If you know of a relevant reference for Aprepitant, please let us know.
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关键词: Aprepitant, Aprepitant supplier, human, substance, P/neurokinin, 1, NK1, hNK1, antagonists, antagonism, tachykinin, receptors, P, SP, antiemetics, CNS, penetrant, orally, bioavailable, Receptor, 6486, Tocris Bioscience
1 篇 Aprepitant 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Aprepitant 的部分引用包括：
Veronica A et al (2022) Dopamine D2 receptors bidirectionally regulate striatal enkephalin expression: Implications for cocaine reward. Cell Rep 40 111440 PMID: 36170833
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Aprepitant 的评论
平均评分: 5 (Based on 1 Review.)
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Very good product.
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Anonymous on 11/19/2020
分析类型： In Vivo
种属： Mouse
In vivo, solution formulation
该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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