Nav1.8-IN-7 (Example 116) is a selective Nav1.8 inhibitor. Nav1.8-IN-7 showed >50% inhibition of Nav1.8 at 100 nM. Nav1.8-IN-7 inhibited hERG with an IC50 of 15.6 μM. Nav1.8-IN-7 has the potential to be used in pain research.

Physicochemical Properties

Molecular Formula	C22H18CLF4N3O5
Molecular Weight	515.84
CAS #	2761181-58-0
Appearance	Typically exists as solid at room temperature
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Nav1.8-IN-9 (Example 116; 1 μM) showed inhibition rates of 1.2%, 3.7%, <1%, <1%, 2.6%, <1% on Nav1.1, Nav1.3, Nav1.4, Nav1.5, Nav1.6, and Nav1.7, respectively [1].
ln Vivo	Pharmacokinetic Parameters of Nav1.8-IN-7 in male Sprague-Dawley rats[1]. PO (100 mg/kg) Cmax (ng/mL) 2566 AUC0-24 (ng/mL∗h) 42454 t1/2 (h ) 8.7
References	[1]. A benzylamine or benzyl alcohol derivative and its use. CN114031518A.

Solubility Data

Solubility (In Vitro)	May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)	The test compound was suspended in 5% DMSO + 95% saline and prepared into a drug delivery system after vortexing for 2 minutes and ultrasonication for 5 minutes. (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9386 mL	9.6929 mL	19.3859 mL
	5 mM	0.3877 mL	1.9386 mL	3.8772 mL
	10 mM	0.1939 mL	0.9693 mL	1.9386 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.