NaV

Nav1.1 activator 1 (compound 4) is an effective Nav1.1 agonist with blood-brain barrier permeability, exhibiting significant selectivity for Nav1.2, Nav1.5, and Nav1.6. It increases the decay time constant of Nav1.1 at 0.03 μM current and can be used for studying central nervous system disorders.

Nav1.7-IN-6, a selective inhibitor of Nav1.7.

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

Nav1.7-IN-2 is avoltage-gated sodium channels (Nav) inhibitor in particular Nav 1.7(IC50 of 80 nM).

Nav1.7-IN-3 is a selective and orally bioavailable inhibitor of voltage-gated sodium channel Nav1.7(IC50 of 8 nM).

Nav1.7 inhibitor is a Nav1.7 inhibitor for research in the field of pain and anesthesia.

NAV26 is a selective blocker of the Nav1.7 channel.

NaV1.7 Blocker-801 is a potent NaV1.7 blocker.

Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.

NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.

AMTB hydrochloride (AMTB HCl) is a novel TRPM8 channel blocker and is effective for pain and urinary diseases. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

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.

Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am

Nav1.8-IN-16 (Compound (R)-40) is an orally bioavailable and selective hNaV 1.8 inhibitor with an IC50 of 5.9 nM. It provides analgesic effects by blocking the NaV1.8 channel without significantly affecting other NaV subtypes or the hERG channel. Nav1.8-IN-16 demonstrates dose-dependent pain relief in postoperative and inflammatory pain models and is suitable for pain-related research.

Nav1.7 blocker 1 (example 41), an effective Na+ channel (Na v) blocker, exhibits a potent IC50 value of 0.037 μM. This compound is utilized in pain research, encompassing neuropathic, postoperative, and inflammatory pain among others [1].

Nav1.7-IN-18 (Compound 31) is a Nav1.7 inhibitor with a Ki value of 4.9 nM and an IC50 of 13 nM, demonstrating analgesic effects in transgenic mice with inherited erythromelalgia (IEM).

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

Nav1.2-IN-1 (compound 5i) is a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative that acts as a potent and selective Nav1.2 inhibitor. It effectively reduces the peak current of Nav1.2 with an IC50 of 7.79 μM. Nav1.2-IN-1 demonstrates antiepileptic activity and shows strong anticonvulsant effects with low neurotoxicity in a subcutaneous pentylenetetrazol (sc-PTZ) induced seizure model.

Nav1.8-IN-6 (Compound 2j) is a novel pyridinone amide Nav1.8 channel inhibitor with IC50 values of 513.33 nM in the resting state and 471.81 nM in the partially activated state. Nav1.8-IN-6 also exhibits analgesic activity.

Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that notably suppresses Veratridine-induced neuronal activity. It inhibits the total Na+ current in DRG neurons in a concentration-dependent manner and delays the activation of Navs. Nav1.7-IN-13 significantly alleviates mechanical pain behavior in a rat model of nerve injury (SNI), exhibiting analgesic properties.

Nav1.8-IN-15 (compound 6) is a potent inhibitor of Nav1.8. It exhibits analgesic properties and holds potential for research in chronic pain management.

At a concentration of 10 μM, Nav1.7 IN WN22(Compound WN22) can achieve an inhibition rate of 80.20% on the hNav1.7 receptor.

Nav1.2-IN-2 (Compound 1) is an effective Nav1.2 inhibitor with an IC₅₀ of 0.18 μM for inactivated Nav1.2. Nav1.2-IN-2 suppresses the amplitude and frequency of spontaneous synchronized calcium oscillations (SCO) and inhibits Veratridine-induced calcium influx (IC₅₀ = 1.89 μM), making it suitable for epilepsy research.

Nav1.8-IN-19 (Compound 122) is a potent inhibitor of Nav1.8.