human nav1.7

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379, an orally active and selective sulfonamide NaV1.7 antagonist.

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.

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

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

PF-05241328 is an effective and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (IC50: 31 nM).

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

PF-04856264 is a Nav1.7 blocker.Nav1.7 is a chondrocyte modulator and a therapeutic target in osteoarthritis.Inhibition of Nav1.7 modulates intracellular Ca 2+ signaling and chondrocyte secretome, raises the threshold of mechanical pain and inhibits ERK expression, which has analgesic and anti-inflammatory effects.

GDC-0310 is a selective acyl-sulfonamide inhibitor targeting the Na_v1.7 channel, with a potent inhibitory concentration (IC_50) of 0.6 nM against hNa_v1.7.

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.

SUN49199, also known as NaV1.7 Blocker-13, is a novel selective blocker of NaV1.7 with little affinity for NaV 1.2, 1.3, or 1.6, being more potent at human vs guinea pig NaV1.7. SUN49199 was reported in Journal of Pharmacology and Experimental Therapeutics (2017), 361(1), 172-180. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https: www.medkoo.com page naming).

PF-05150122 is a novel potent and selective human Nav1.7 blocker.

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.

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

Cd1a, a β-toxin from the African spider Ceratogyrus darlingi, modulates calcium ion channels and inhibits human calcium ion channels (Ca v 2.2)(IC 50 2.6 μM) as well as mouse sodium ion channels (Na v 1.7). This compound has potential applications in creating drugs for the treatment of peripheral pain [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.

DS43260857 is a potent NaV1.7 inhibitor with high inhibitory effects on both human and mouse NaV1.7, exhibiting IC50 values of 6.6 μM for hNaV1.1, 14 μM for hNaV1.5, 0.015 μM for hNaV1.7, and 0.061 μM for mNaV1.7 [1].

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases

GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).