Nav1.8-IN-24 

Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC₅₀ values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain^[1].

Nav1.8-IN-24 (Compound 24) potently and selectively inhibits NaV1.8 channels in HEK cells, with pIC₅₀ values of 7.4 (resting state) and 7.5 (inactivated state), and negligible activity against other NaV isoforms (pIC₅₀ < 4.5)^[1].
Nav1.8-IN-24 shows low metabolic clearance in human and rat liver microsomes and hepatocytes, indicating favorable metabolic stability^[1].
Nav1.8-IN-24 has moderate Caco-2 permeability, low PXR activation, no significant CYP inhibition, and negligible activity against key cardiac ion channels, indicating a favorable early in vitro safety profile^[1].

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

Nav1.8-IN-24 (Compound 24) (1-10 mg/kg; i.v.; p.o.) demonstrates an extended in vivo half-life of ^13.9 h in rats and achieves an unbound DRG-to-plasma partition coefficient of 0.72, indicating favorable exposure in the pain-relevant target tissue^[1].

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

453.37

C₂₀H₁₆F₅N₅O₂

O=C(N1C[C@@H](O[C@@H](C1)C(F)(F)F)C2=C(C=CC=C2F)F)NC3=CN(N=N3)C4=CC=CC=C4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Dialer C, et al. Discovery and Optimization of Potent and Subtype-Selective Urea-Derived Na_V1.8 Inhibitors. ACS Med Chem Lett. 2026;17(5):1179-1188. Published 2026 May 1.  [Content Brief]