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Submit ReviewSB 452533 is a potent TRPV1 antagonist against capsaicin (pKb = 7.7), noxious heat and acid-mediated (pIC50 = 7.0) receptor activation (pKi = 6.22 at the recombinant hTRPV1 receptor). Exhibits analgesic properties.
Sold for research purposes only under agreement from GlaxoSmithKline
分子量 | 376.29 |
公式 | C18H22BrN3O |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 459429-39-1 |
PubChem ID | 9842609 |
InChI Key | IFJYEGJUQIBBQV-UHFFFAOYSA-N |
Smiles | CC1=CC(N(CC)CCNC(NC2=CC=CC=C2Br)=O)=CC=C1 |
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.
参考文献是支持产品生物活性的出版物。
Rami et al (2004) Discovery of small molecule antagonists of TRPV1. Bioorg.Med.Chem.Lett. 14 3631 PMID: 15203132
Weil et al (2005) Conservation of functional and pharmacological properties in the distantly related temperature sensors TRPV1 and TRPM8. Mol.Pharmacol. 68 518 PMID: 15911692
Bianchi et al (2007) [3H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-ylurea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J.Pharmacol.Exp.Ther. 323 285 PMID: 17660385
关键词: SB 452533, SB 452533 supplier, SB452533, TRPV1, transient, receptor, potential, channels, antagonists, vanilloid, receptors, analgesic, analgaesic, TRPV, 3265, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SB 452533 的部分引用包括:
Vijayvergiya et al (2015) Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. Mol Pain 10 e0141366 PMID: 26513481
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