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| 化学名: | | | 英語化学名: | CVN293 | | 别名: | CVN293;4-(7-Fluoro-1-(pyridazin-3-ylmethyl)-1H-benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine | | CAS番号: | 2815296-08-1 | | 分子式: | | | 分子量: | 0 | | EINECS: | | | カテゴリ情報: | | | Mol File: | Mol File | ![CVN293]() |
| 外見 | Solid | | 色 | White to light yellow |
| | CVN293 Usage And Synthesis |
| 使用 | CVN293 is a selective and brain permeable potassium ion (K+) channel KCNK13 inhibtor with IC50s of 41 nM and 28 nM for hKCNK13 and mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome mediated production of the proinflammatory cytokine IL-1β in microglia[1]. | | in vivo | Pharmacokinetic Parameters of CVN293 in male Sprague-Dawley rat, dog and cynomolgus monkey[1].
| IV (0.5 mg/kg; rat) | PO (3 mg/kg; rat) | IV (1 mg/kg; dog) | PO (10 mg/kg; dog) | IV (1 mg/kg; cynomolgus monkey) | PO (3 mg/kg; cynomolgus monkey) | | Tmax (h) | | 1.0 | | 1.25 | | 1.0 | | Cmax (ng/mL) | | 468 | | 241 | | 165 | | AUC0-∞ (ng?h/mL) | 222 | 1236 | 438 | 630 | 782 | 546 | | t1/2 (h) | 1.0 | 2.0 | 0.5 | 2.6 | 1.1 | 1.9 | | CLp (mL/min/kg) | 35 | | 38 | | 22 | | | Vss (L/kg) | 1.85 | | 1.42 | | 1.45 | | | F (%) | | 87 | | 41 | | 24 |
| | IC 50 | hKCNK13: 41 nM (IC50); mKCNK13: 28 nM (IC50); hKCNK6: >30000 nM (IC50); hKCNK2: >30000 nM (IC50) | | 参考文献 | [1] Roland W. Bürli, et al.Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment. ACS Med. Chem. Lett. 2024. |
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