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ebselen
| Compound Class | Synthetic organic |
|---|---|
| 变动原因 |
A synthetic organoselenium molecule with anti-inflammatory, anti-oxidant and cytoprotective activity, characterised as a small molecule Gq protein inhibitor. A bioRxiv preprint suggests that ebselen is a low micromolar, covalent, fast-binding inhibitor of papain-like protease (PL-pro) from SARS-CoV-2 |
| Related Product | 依布硒 |
Summary
| 是否批准为药物？ | |
|---|---|
| IUPAC Name | 2-phenyl-1,2-benzoselenazol-3-one |
生物活性
| 生物活性评价 |
Ebselen completely blocked Carbachol-induced calcium mobilization (via the Gq-coupled muscarinic M3 receptor) as well as ADP-induced calcium mobilization (via the P2Y1 receptor) in recombinant 1321N1 astrocytoma cells with pIC50 values of 5.36 and 5.63, respectively |
|---|---|
| 关联靶标 | CoV Papain-like protease |
临床资料
| 作用机制与药效学效应 |
Sulfonamides are structural analogues of 4-aminobenzoic acid (pABA) an intermediate in the de novo synthesis of folate by some prokaryotes, lower eukaryotes and plants |
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参考文献
| 1. Kuschak M, Namasivayam V, Rafehi M, Voss JH, Garg J, Schlegel JG, Abdelrahman A, Kehraus S, Reher R, Küppers J et al.. (2020) Cell-permeable high-affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors.. Br J Pharmacol, 177 (8): (1898-1916). [PMID:31881095] |
| 2. W?glarz-Tomczak E, Tomczak JM, Talma M, Brul S. (2020) Ebselen as a highly active inhibitor of PLProCoV2. bioRxiv, 71 (13): (1755-70). [PMID:21902297] |
结构
| Canonical SMILES | O=c1c2ccccc2[se]n1c1ccccc1 |
|---|---|
| Isomeric SMILES | O=c1c2ccccc2[se]n1c1ccccc1 |
| InChI | InChI=1S/C13H9NOSe/c15-13-11-8-4-5-9-12(11)16-14(13)10-6-2-1-3-7-10/h1-9H |
| InChI key | DYEFUKCXAQOFHX-UHFFFAOYSA-N |
危险品化学品经营许可证（带存储）