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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

Nav1.7 channel inhibitor

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

10

Peptides

4

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16723
    Funapide

    TV 45070; XEN402

    		 Sodium Channel Neurological Disease Inflammation/Immunology
    Funapide (TV 45070; XEN402) is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
    Funapide
  • HY-103623
    PF-05241328

    		Sodium Channel Neurological Disease
    PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
    PF-05241328
  • HY-100727
    AM-2099

    		Sodium Channel Neurological Disease
    AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
    AM-2099
  • HY-P1221A
    ProTx II TFA

    		Sodium Channel Neurological Disease
    ProTx II TFA is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors .
    ProTx II TFA
  • HY-12796
    Raxatrigine

    Vixotrigine; GSK-1014802; CNV1014802

    		 Sodium Channel Neurological Disease
    Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
    Raxatrigine
  • HY-12796A
    Raxatrigine hydrochloride

    Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride

    		 Sodium Channel Neurological Disease
    Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
    Raxatrigine hydrochloride
  • HY-112279
    GNE-131

    		Sodium Channel Neurological Disease
    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
    GNE-131
  • HY-12811
    PF-04856264

    		Sodium Channel Neurological Disease
    PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
    PF-04856264
  • HY-101789
    Nav1.7-IN-3

    		Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
    Nav1.7-IN-3
  • HY-P1221
    ProTx II

    		Sodium Channel Neurological Disease
    ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors .
    ProTx II
  • HY-119934
    NaV1.7 inhibitor-1

    		Sodium Channel Neurological Disease
    NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5 .
    NaV1.7 inhibitor-1
  • HY-167852
    GX-585

    		Others Neurological Disease Inflammation/Immunology
    GX-585 is a sulfonamide analog that acts as a Nav1.7 channel inhibitor, demonstrating analgesic activity in treating neuropathic pain and inflammation.
    GX-585
  • HY-155236
    Ancistrotecine B

    		Sodium Channel Inflammation/Immunology
    Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice .
    Ancistrotecine B
  • HY-122001
    PF-05186462

    		Sodium Channel Neurological Disease
    PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC50 of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain .
    PF-05186462
  • HY-P5793
    GTx1-15

    		Sodium Channel Calcium Channel Neurological Disease
    GTx1-15 is an inhibitor cystine knot (ICK) peptide that inhibits the voltage-dependent calcium channel Cav3.1 and the voltage-dependent sodium channels Nav1.3 and Nav1.7 .
    GTx1-15
  • HY-162609
    ST-2560

    		Sodium Channel Cardiovascular Disease Neurological Disease
    ST-2560 is a selective inhibitor of the NaV1.7 sodium channel with IC50 value of 39 nM. ST-2560 can be used to study pain behavior and cardiovascular models .
    ST-2560
  • HY-N6691
    Veratridine
    3 Publications Verification

    3-Veratroylveracevine

    		 Sodium Channel Neurological Disease
    Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow .
    Veratridine
  • HY-16723A
    (R)-Funapide

    (R)-TV 45070; (R)-XEN402

    		 Sodium Channel Neurological Disease Inflammation/Immunology
    (R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
    (R)-Funapide
  • HY-123833
    PF-05661014

    		Sodium Channel Others
    PF-05661014, a desmethyl analogue of PF-06526290, selectively inhibits Nav1.3 and Nav1.7 currents by stabilizing inactivated channels via interaction with D4 VSD. PF-05661014 can be used for research of sodium channel modulation .
    PF-05661014
  • HY-N1847
    3'-Methoxydaidzein

    		Sodium Channel Neurological Disease
    3'-Methoxydaidzein is a isoflavone and a Sodium Channel inhibitor. 3'-Methoxydaidzein inhibits subtypes NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM, and 505 nM, respectively. 3'-Methoxydaidzein exerts analgesic activity by inhibiting voltage-gated sodium channels .
    3'-Methoxydaidzein
  • HY-P1220
    Huwentoxin-IV

    		Sodium Channel Neurological Disease
    Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
    Huwentoxin-IV
  • HY-P1220A
    Huwentoxin-IV TFA

    		Sodium Channel Neurological Disease
    Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
    Huwentoxin-IV TFA
  • HY-128794
    PF-05150122

    		Others Neurological Disease
    PF-05150122 is a novel potent and selective human Nav1.7 channel blocker with the activity of inhibiting human pain signaling. PF-05150122 exhibited favorable biopharmacokinetic parameters in microdose studies, providing a basis for exploring its application in acute or chronic pain inhibition. The pharmacokinetic model of PF-05150122 predicted that at the corresponding oral dose, it could effectively reduce the 50% inhibitory concentration (IC50) of Nav1.7, demonstrating its inhibitory potential .
    PF-05150122
  • HY-P5865
    Tap1a

    Theraphotoxin-Tap1a; TRTX-Tap1a; µ/ω-TRTX-Tap1a

    		 Sodium Channel Neurological Disease
    Tap1a (Theraphotoxin-Tap1a) is a spider venom peptide that inhibits sodium channels with IC50s of 80 nM and 301 nM against Nav1.7 and Nav1.1, respectively. Tap1a shows analgesic effects .
    Tap1a
  • HY-P5160
    Phlotoxin-1

    PhlTx1

    		 Sodium Channel Inflammation/Immunology
    Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel .
    Phlotoxin-1
  • HY-N6691R
    Veratridine (Standard)

    		Sodium Channel Neurological Disease
    Veratridine (Standard) is the analytical standard of Veratridine. This product is intended for research and analytical applications. Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39?μM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow .
    Veratridine (Standard)
  • HY-108425A
    AMG8380

    		Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
    AMG8380
  • HY-135495
    AM-0466

    		Sodium Channel Histamine Receptor Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466
  • HY-P5153
    ProTx-III

    μ-TRTX-Tp1a

    		 Sodium Channel Neurological Disease
    ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
    ProTx-III
  • HY-19366
    Nav1.7-IN-2

    		Sodium Channel Neurological Disease
    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
    Nav1.7-IN-2
  • HY-107405
    TC-N 1752

    		Sodium Channel Neurological Disease
    TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain .
    TC-N 1752
  • HY-P5790
    μ-TRTX-Hd1a

    		Sodium Channel Neurological Disease
    μ-TRTX-Hd1a, a spider venom, is a selective NaV 1.7 inhibitor. μ-TRTX-Hd1a is a gating modifier that inhibits human NaV 1.7 by interacting with the S3b-S4 paddle motif in channel domain II .
    μ-TRTX-Hd1a
  • HY-162347
    Nav1.7-IN-13

    		Sodium Channel Neurological Disease
    Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
    Nav1.7-IN-13
  • HY-123824
    GNE-0439

    		Sodium Channel Neurological Disease
    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .
    GNE-0439
  • HY-157802
    LTGO-33

    		Sodium Channel Neurological Disease
    LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
    LTGO-33

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