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Submit ReviewAMG 21629 is a potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors (IC50 values are 0.6 and 0.8 nM for capsaicin (Cat. No. 0462) and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant.
分子量 | 472.42 |
公式 | C22H19F3N6O3 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 939040-79-6 |
PubChem ID | 24858024 |
InChI Key | TUMYQRZCVIQKOQ-UHFFFAOYSA-N |
Smiles | NC(C(N4)=O)=NC(C4=CC=C3)=C3OC1=CC(C2=CC=C(C(F)(F)F)C=C2)=NC(NCCOC)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 23.62 | 50 |
以下数据基于产品分子量 472.42。 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 | 4.23 mL | 21.17 mL | 42.34 mL |
2.5 mM | 0.85 mL | 4.23 mL | 8.47 mL |
5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
25 mM | 0.08 mL | 0.42 mL | 0.85 mL |
参考文献是支持产品生物活性的出版物。
Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID: 18386885
Gavva et al (2007) The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J.Neurosci. 27 3366 PMID: 17392452
If you know of a relevant reference for AMG 21629, please let us know.
关键词: AMG 21629, AMG 21629 supplier, AMG21629, transient, receptor, potential, vanilloid, TRPV1, antagonists, antagonism, orally, available, potent, selective, hyperthermia, TRPV, 4330, Tocris Bioscience
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