nav1.8 channel

Suzetrigine(VX-548) is an orally active and specific NaV1.8 inhibitor. Suzetrigine has analgesic activity and can be used to study acute pain and neurotransmission.

Nav1.8-IN-4 is a potent Nav1.8 channel inhibitor with potential analgesic activity.Nav1.8-IN-4 can be used for pain and neurological related disorders.

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.

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM).

Cyfluthrin binds to voltage-sensitive sodium channel such as Nav 1.8 sodium channel and modify their gating kinetics, thereby disrupting nerve function of pests.

A-803467 is a selective NaV1.8 channel blocker.

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker [IC50: 196 nM].

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

KGP-25 is an inhibitor of the voltage-gated sodium channel 1.8 (Nav1.8), utilized for analgesia by targeting the peripheral nervous system (PNS). Additionally, it targets the γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for use as a general anesthetic.

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].

VSTx-3 is a potassium voltage-gated channel (K_V) blocker, which has also been shown to be a potent tetrodotoxin-sensitive (TTX-sensitive) sodium channel inhibitor, with particular efficacy against NaV1.8 channels, as evidenced by its half-maximal inhibitory concentration (IC_50) values of 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7, and 0.77 μM for hNaV1.8 channels.

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].

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.

Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels.

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.

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].

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.

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.

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

Acid-sensing ion channel 3 (ASIC3) channel blocker (IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against

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