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Submit ReviewJNJ 17203212
说明： Reversible, competitive and potent TRPV1 antagonist
化学名： 4-[3-(Trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide
纯度： ≥99% (HPLC)
生物活性 for JNJ 17203212
JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist (pKi values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H+-induced channel activation (pIC50 values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo.
化合物库 for JNJ 17203212
JNJ 17203212 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 JNJ 17203212
| 分子量 | 419.32 |
| 公式 | C17H15F6N5O |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 821768-06-3 |
| PubChem ID | 11339118 |
| InChI Key | JFRYYGVYCWYIDQ-UHFFFAOYSA-N |
| Smiles | O=C(NC3=NC=C(C(F)(F)F)C=C3)N(CC2)CCN2C1=C(C(F)(F)F)C=CC=N1 |
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 JNJ 17203212
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.93 | 100 | |
| ethanol | 41.93 | 100 |
制备储备液 for JNJ 17203212
以下数据基于产品分子量 419.32。 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 | 2.38 mL | 11.92 mL | 23.85 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for JNJ 17203212
参考文献 for JNJ 17203212
参考文献是支持产品生物活性的出版物。
Swanson et al (2005) Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J.Med.Chem. 48 1857 PMID: 15771431
Ghilardi et al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126 PMID: 15788769
Bhattacharya et al (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J.Pharmacol.Exp.Ther. 323 665 PMID: 17690251
If you know of a relevant reference for JNJ 17203212, please let us know.
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关键词: JNJ 17203212, JNJ 17203212 supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, TRPV, 3361, Tocris Bioscience
2 篇 JNJ 17203212 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JNJ 17203212 的部分引用包括：
Kelly et al (2015) Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain. PLoS One 74 252 PMID: 24152419
Vijayvergiya et al (2015) Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. PLoS One 10 e0141366 PMID: 26513481
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