nav1.7/nav1.8

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

(R)-DSP-2230 is the R-isomer of DSP-2230. DSP-2230 is a selective blocker of Nav1.7 Nav1.8.

ABBV-318 can be used as small molecule Nav1.7 Nav1.8 blockers for the treatment of pain, with IC50 values of 2.8 μM for hNav1.7 and 3.8 μM for hNav1.8. ABBV-318 can be used to study pain-related disorders.

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 &#181M for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, inhibits Kv4.2 and Nav1.7 currents while activating Nav1.9 channels, with no effect on Nav1.8 channels [1].

3'-Methoxydaidzein is a dual isoflavone and Sodium Channel inhibitor. 3'-Methoxydaidzein inhibited NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM and 505 nM, respectively. 3'-Methoxydaidzein was specific for collagen-induced platelet aggregation with IC50 values of 12.3 and 61.5µM, respectively. 3'-Methoxydaidzein acts as an analgesic by inhibiting voltage-gated sodium channels. 3'-Methoxydaidzein showed antioxidant activity and antiplatelet aggregation activity.

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

DSP-2230 is a selective blocker of Nav1.7 Nav1.8.