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Cat. No.: HY-183709

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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.

For research use only. We do not sell to patients.

Formula: C₂₀H₁₆F₅N₅O₂
Molecular Weight:453.37

Storage:

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

Nav1.8-IN-24 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

Na_v1.8

7.4 (pIC₅₀)

Na_v1.8

7.5 (pIC₅₀)

All Sodium Channel Isoforms :

In Vitro

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.

Parmacokinetics

Species	Dose	Route	V_dss	CL	CL_unbound	T_1/2	T_max	C_max	AUC_0-t	Bioavailability
Rat^[1]	1 mg/kg	i.v.	3.23 L/kg	2.94 mL/min/kg	1176 mL/min/kg	13.9 h	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	/	/	/	16.6 h	4.0 h	0.36 μM	5.44 μM·h	6 %

In Vivo

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.

Chemical Information

Molecular Weight 453.37
Formula C₂₀H₁₆F₅N₅O₂
SMILES

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
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

Handling Instructions (2659 KB)

References

[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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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