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CVN293
CAS No. : 2815296-08-1
MCE 國際站：CVN293
產(chǎn)品活性：CVN293 是一種選擇性的，能夠透過血腦屏障的鉀離子 (K+) 通道 KCNK13 抑制劑，對 hKCNK13 和 mKCNK13 的 IC50 值分別為 41 nM 和 28 nM。CVN293 有效抑制小膠質細胞中 NLRP3 炎癥小體介導的促炎細胞因子 IL-1β 的產(chǎn)生。
研究領域：Membrane Transporter/Ion Channel | Immunology/Inflammation
作用靶點：Potassium Channel | NOD-like Receptor (NLR)
In Vitro: CVN293 (0.05, 0.5, 5 μM) demonstrates a concentration-dependent inhibition of the NLRP3-inflammasome mediated production of IL-1β from LPS-primed murine microglia.
In Vivo: Pharmacokinetic Parameters of CVN293 in male Sprague-Dawley rat, dog and cynomolgus monkey.
| 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-∞ (ngh/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 |
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