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Submit ReviewRS 127445 hydrochloride
说明： High affinity and selective 5-HT2B antagonist
别名： MT 500
化学名： 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine hydrochloride
纯度： ≥98% (HPLC)
生物活性 for RS 127445 hydrochloride
RS 127445 hydrochloride is a high affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.
化合物库 for RS 127445 hydrochloride
RS 127445 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for RS 127445 hydrochloride
| 分子量 | 317.79 |
| 公式 | C17H16FN3.HCl |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 199864-86-3 |
| PubChem ID | 9905058 |
| InChI Key | MKJPYBJBPRFMHL-UHFFFAOYSA-N |
| Smiles | FC1=C(C=CC=C2)C2=C(C3=CC(C(C)C)=NC(N)=N3)C=C1.Cl |
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 RS 127445 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.78 | 100 | |
| ethanol | 31.78 | 100 |
制备储备液 for RS 127445 hydrochloride
以下数据基于产品分子量 317.79。 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 | 3.15 mL | 15.73 mL | 31.47 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.29 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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产品说明书 for RS 127445 hydrochloride
参考文献 for RS 127445 hydrochloride
参考文献是支持产品生物活性的出版物。
Bonhaus et al (1999) RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br.J.Pharmacol. 127 1075 PMID: 10455251
Callebert et al (2006) Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine2B receptors in mice. J.Pharmacol.Exp.Ther. 317 724 PMID: 16461587
If you know of a relevant reference for RS 127445 hydrochloride, please let us know.
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关键词: RS 127445 hydrochloride, RS 127445 hydrochloride supplier, Selective, high, affinity, 5-HT2B, antagonists, Serotonin, Receptors, RS127445, hydrochloride, MT500, MT, 500, 2993, Tocris Bioscience
8 篇 RS 127445 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 RS 127445 hydrochloride 的部分引用包括：
Söhle et al (2012) Identification of new genes involved in human adipogenesis and fat storage. PLoS One 7 e31193 PMID: 22384002
Lofdahl (2018) Pulmonary fibrosis in vivo displays increased p21 expression reduced by 5-HT2B receptor antagonists in vitro - a potential pathway affecting proliferation. Sci Rep 8 1927 PMID: 29386571
Palmqvist et al (2016) A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030. J Inflamm (Lond) 13 20 PMID: 27340371
Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000
Chabbi-Achengli et al (2013) Serotonin 2B receptor (5-HT2B R) signals through prostacyclin and PPAR-β/δ in osteoblasts. PLoS One 8 e75783 PMID: 24069449
Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217
Banas et al (2011) Deconstructing antiobesity compound action: requirement of serotonin 5-HT2B receptors for dexfenfluramine anorectic effects. Neuropsychopharmacology 36 423 PMID: 20927048
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.