1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. CVN293

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.

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CVN293 Chemical Structure

CVN293 Chemical Structure

CAS No. : 2815296-08-1

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Description

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].

IC50 & Target[1]

hKCNK13

41 nM (IC50)

mKCNK13

28 nM (IC50)

hKCNK6

>30000 nM (IC50)

hKCNK2

>30000 nM (IC50)

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

311.27

Formula

C14H10FN7O

CAS No.
Unlabeled Cas

SMILES

NC1=NON=C1C2=NC3=CC=CC(F)=C3N2CC4=NN=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CVN293 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CVN293
Cat. No.:
HY-158155
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