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Submit ReviewAMG 517 is a potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.
AMG 517 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 430.41 |
公式 | C20H13F3N4O2S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 659730-32-2 |
PubChem ID | 16007367 |
InChI Key | YUTIXVXZQIQWGY-UHFFFAOYSA-N |
Smiles | O=C(NC(S1)=NC(C1=CC=C2)=C2OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 4.3 | 10 |
以下数据基于产品分子量 430.41。 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 |
---|---|---|---|
0.1 mM | 23.23 mL | 116.17 mL | 232.34 mL |
0.5 mM | 4.65 mL | 23.23 mL | 46.47 mL |
1 mM | 2.32 mL | 11.62 mL | 23.23 mL |
5 mM | 0.46 mL | 2.32 mL | 4.65 mL |
参考文献是支持产品生物活性的出版物。
Gavva et al (2007) Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J.Pharmacol.Exp.Ther. 323 128 PMID: 17652633
Wang et al (2007) Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J.Med.Chem. 50 3528 PMID: 17585751
Doherty et al (2007) Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J.Med.Chem. 50 3515 PMID: 17585750
If you know of a relevant reference for AMG 517, please let us know.
关键词: AMG 517, AMG 517 supplier, AMG517, potent, TRPV1, transient, potential, channels, antagonists, pain, antihyperalgesia, TRPV, 5995, Tocris Bioscience
平均评分: 5 (Based on 1 Review.)
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