2815296-08-1

Name	CVN293
CAS	2815296-08-1

Synonyms

CVN293 4-(7-Fluoro-1-(pyridazin-3-ylmethyl)-1H-benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine

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Chemical Properties

form	Solid
color	White to light yellow

Hazard Information

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)
T_max (h)		1.0		1.25		1.0
C_max (ng/mL)		468		241		165
AUC_0-∞ (ng?h/mL)	222	1236	438	630	782	546
t_1/2 (h)	1.0	2.0	0.5	2.6	1.1	1.9
CLp (mL/min/kg)	35		38		22
V_ss (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.

Supplier

Foshan Heshuo Pharm technology Co., ltd

Telephone 15363639686

Websitehttp://www.hs-pharm.cn

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Shaanxi Kebele Pharmaceutical R&D Co., Ltd

Telephone13119135307 13119135307

Website

Shanghai Mumin Biotechnology Co., Ltd

Telephone17177768578 17177768578

Websitehttps://www.chemicalbook.com/supplier/134305340/

Cayman Chemical Company

Telephone800-364-9897

Websitehttp://www.caymanchem.com

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