CVN293
- CAS No.
- 2815296-08-1
- Chemical Name:
- CVN293
- Synonyms
- CVN293;4-(7-Fluoro-1-(pyridazin-3-ylmethyl)-1H-benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine
- CBNumber:
- CB414253654
- Molecular Formula:
- Molecular Weight:
- 0
- MDL Number:
- MOL File:
- Mol file
CVN293 Chemical Properties,Uses,Production
Uses
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)
References
[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.
CVN293 Preparation Products And Raw materials
Raw materials
Preparation Products
CVN293 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Foshan Heshuo Pharm technology Co., ltd | 15363639686 | heshuoyiyao@hotmail.com | China | 1028 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19727 | 58 |
| Shaanxi Kebele Pharmaceutical R&D Co., Ltd | 13119135307 13119135307 | 3866620171@qq.com | China | 2063 | 58 |
| Shanghai Mumin Biotechnology Co., Ltd | 17177768578 17177768578 | alisa@pemichem.com | China | 427 | 58 |