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Submit ReviewL-733,060 hydrochloride
说明： Potent NK1 antagonist
化学名： (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
纯度： ≥99% (HPLC)
生物活性 for L-733,060 hydrochloride
L-733,060 hydrochloride is a potent NK1 antagonist (Ki values are 0.08, 0.2 and 93.13 nM for gerbil, human and rat receptors, respectively). Produces anxiolytic-like effects in the gerbil elevated plus-maze. Exhibits antitumor activity in vitro. Also decreases HER2 activity and tumor growth in mice bearing HER2+ or EGFR+ breast tumors. Orally bioavailable and brain penetrant.
许可信息
Sold with the permission of Merck, Sharpe and Dohme Ltd.
技术数据 for L-733,060 hydrochloride
| 分子量 | 439.83 |
| 公式 | C20H19F6NO.HCl |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 148687-76-7 |
| PubChem ID | 11957600 |
| InChI Key | DYEUTIUITGHIEO-APTPAJQOSA-N |
| Smiles | Cl[H].FC(F)(F)C1=CC(=CC(CO[C@H]2CCCN[C@H]2C2=CC=CC=C2)=C1)C(F)(F)F |
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 L-733,060 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 21.99 | 50 温和加热 |
制备储备液 for L-733,060 hydrochloride
以下数据基于产品分子量 439.83。 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 |
|---|---|---|---|
| 0.5 mM | 4.55 mL | 22.74 mL | 45.47 mL |
| 2.5 mM | 0.91 mL | 4.55 mL | 9.09 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.55 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.91 mL |
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产品说明书 for L-733,060 hydrochloride
参考文献 for L-733,060 hydrochloride
参考文献是支持产品生物活性的出版物。
Kramer et al (1998) Distinct mechanism for antidepressant blockade of central substance P receptors. Science 281 1640 PMID: 9733503
Seabrook et al (1996) L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur.J.Pharmacol. 317 129 PMID: 8982729
Varty et al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371 PMID: 12225694
Garcia-Recio et al (2013) Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer. Cancer Res. 73 6424 PMID: 24030979
If you know of a relevant reference for L-733,060 hydrochloride, please let us know.
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关键词: L-733,060 hydrochloride, L-733,060 hydrochloride supplier, Potent, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L733060, Receptor, 1145, Tocris Bioscience
15 篇 L-733,060 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-733,060 hydrochloride 的部分引用包括：
D'Amato et al (2015) A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer. Cancer Res 75 4651 PMID: 26363006
García-Recio et al (2015) The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation. PLoS One 10 e0129661 PMID: 26114632
Muschter et al (2019) Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages. Int J Mol Sci 20 PMID: 30682804
Khasabov et al (2017) Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla. J Neurophysiol 118 2727 PMID: 28794197
Fong et al (2017) The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1. PLoS One 12 e0174101 PMID: 28301610
Bang et al (2004) Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage. Br J Sports Med 308 1174 PMID: 14617692
Backman et al (2014) Substance P reduces TNF-α-induced apoptosis in human tenocytes through NK-1 receptor stimulation. Mol Cancer Res 48 1414 PMID: 23996004
Nassini et al (2010) Acetaminophen, via its reactive metabolite N-acetyl-p-benzo-quinoneimine and transient receptor potential ankyrin-1 stimulation, causes neurogenic inflammation in the airways and other tissues in rodents. FASEB J 24 4904 PMID: 20720158
Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. PLoS One 294 R1517 PMID: 18337316
Gupta et al (2007) Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol 375 29 PMID: 17295025
Sloniecka et al (2016) Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8. Mol Pharmacol 89 215 PMID: 26646648
Zhang et al (2008) Sprouting of substance P-expressing primary afferent central terminals and spinal micturition reflex NK1 receptor dependence after spinal cord injury. Am J Physiol Regul Integr Comp Physiol 295 R2084 PMID: 18945947
Nassini et al (2012) Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation. Oncotarget 7 e42454 PMID: 22905134
Li et al (2013) Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells. Am J Physiol Regul Integr Comp Physiol 11 294 PMID: 23345604
Liu et al (2013) TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J 27 3549 PMID: 23722916
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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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