nav1.8 in 1

Nav1.8 modulator 1 (compound 1) is an effective modulator of Nav1.8, showing potential for pain research.

Nav1.8-IN-11 (Example 1), a Nav1.8 channel inhibitor with an IC50 of 0.1 nM, is utilized in research on pain disorders [1].

Nav1.8-IN-12 (Compound 23 R) serves as an inhibitor of the Nav1.8 channel and is utilized in the research of pain-related diseases [1].

Nav1.8-IN-13 (compound 16), functioning as a Nav1.8 inhibitor with a pIC50 value of 7.9, is referenced as [1].

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]

PF-06305591 dihydrate is a potent and highly selective voltage-gated sodium channel NaV1.8 blocker (IC50 = 15 nM) with excellent preclinical in vitro ADME and safety profiles [1].

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

Analgesic Agent-2, a selective orally active inhibitor of the NaV1.8 channel, demonstrates an IC50 of 50.18 nM in HEK293 cells that stably express the human NaV1.8 channel, indicating its potential for analgesic activity [1].

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8

Nav1.8-IN-5 (Example 1), a voltage-gated sodium channel Nav1.8 inhibitor, is applicable in the research of Nav1.8-mediated diseases including pain, pain-related disorders, and cardiovascular diseases (such as atrial fibrillation) [1].

Nav1.8-IN-7 (Example 116) serves as a selective inhibitor of Nav1.8, demonstrating more than 50% inhibition at 100 nM specifically for Nav1.8. It exhibits an IC50 of 15.6 μM for the hERG channel. This compound holds promise in the field of pain research [1].

Nav1.8-IN-9 (Example 16), a potent Nav1.8 inhibitor with an IC 50 of 0.084 nM, is orally active and holds promise for extensive pain research [1].