nav1.8 in 1

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

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-10 (Compound 6), functioning as a Nav1.8 channel inhibitor, exhibits a 79.4% blocking rate of the Nav1.8 channel at a concentration of 4 nM. This compound is utilized in researching pain disorders [1].

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].

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-8 (Compound A11), a Nav1.8 channel inhibitor, potentially mitigates diseases mediated by sodium ion channels (NaV) [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].