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CVN293 is a selective and brain-permeable potassium ion (K+) channel KCNK13 inhibitor with IC50 values of 41 nM for hKCNK13 and 28 nM for mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome-mediated production of the pro-inflammatory cytokine IL-1β in microglia [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $67 | In Stock | |
5 mg | $162 | In Stock | |
10 mg | $238 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $579 | In Stock | |
100 mg | $786 | In Stock | |
200 mg | $1,080 | In Stock |
Description | CVN293 is a selective and brain-permeable potassium ion (K+) channel KCNK13 inhibitor with IC50 values of 41 nM for hKCNK13 and 28 nM for mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome-mediated production of the pro-inflammatory cytokine IL-1β in microglia [1]. |
Targets&IC50 | hKCNK2:>30000 nM, hKCNK13:41 nM, hKCNK6:>30000 nM, mKCNK13:28 nM |
In vitro | CVN293 (0.05, 0.5, 5 μM) exhibits a dose-dependent inhibitory effect on LPS-induced IL-1β production in mouse microglial cells mediated by the NLRP3 inflammasome [1]. |
In vivo | Pharmacokinetic Parameters of CVN293 were evaluated in male Sprague-Dawley rats, dogs, and cynomolgus monkeys [1]. In rats, IV (0.5 mg/kg) and PO (3 mg/kg) administration resulted in T_max of 1.0 h, C_max of 468 ng/mL, AUC_0-∞ of 222 ng•h/mL, 1236 ng•h/mL, t_1/2 of 1.0 h and 2.0 h, CLp of 35 mL/min/kg, and V_ss of 1.85 L/kg with F at 87%. In dogs, IV (1 mg/kg) and PO (10 mg/kg) administration yielded a T_max of 1.0 h, C_max of 241 ng/mL, AUC_0-∞ of 438 ng•h/mL, 630 ng•h/mL, t_1/2 of 0.5 h and 2.6 h, CLp of 38 mL/min/kg, and V_ss of 1.42 L/kg with F at 41%. For cynomolgus monkeys, IV (1 mg/kg) and PO (3 mg/kg) resulted in T_max of 1.0 h, C_max of 165 ng/mL, AUC_0-∞ of 782 ng•h/mL, 546 ng•h/mL, t_1/2 of 1.1 h and 1.9 h, CLp of 22 mL/min/kg, and V_ss of 1.45 L/kg with F at 24%. |
Molecular Weight | 311.27 |
Formula | C14H10FN7O |
Cas No. | 2815296-08-1 |
Smiles | C(N1C(=NC=2C1=C(F)C=CC2)C=3C(N)=NON3)C4=CC=CN=N4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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