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Results for "

NAV1 Inhibitors

" in MCE Product Catalog:

35

Inhibitors & Agonists

4

Peptides

1

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-13985
    Nav1.7 inhibitor

    Sodium Channel Neurological Disease
    Nav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain.
  • 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.
  • 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.
  • 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.
  • HY-102998
    Nav1.7-IN-6

    Sodium Channel Neurological Disease
    Nav1.7-IN-6 (example 346) is a Nav1.7 selective inhibitor, which is extracted from patent WO2015078374A1.
  • 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.
  • 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.
  • HY-141547
    Nav1.7-IN-8

    Sodium Channel Cytochrome P450 Inflammation/Immunology
    Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.
  • HY-16723
    Funapide

    TV 45070; XEN402

    Sodium Channel Inflammation/Immunology
    Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
  • 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.
  • 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.
  • 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.
  • HY-131870
    GX-201

    Sodium Channel Inflammation/Immunology
    GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7.
  • HY-12796A
    Raxatrigine 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.
  • HY-12796
    Raxatrigine

    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.
  • HY-128772
    XPC-6444

    Sodium Channel Neurological Disease
    XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.
  • 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.
  • HY-139081
    GDC-0310

    Sodium Channel Neurological Disease
    GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7.
  • 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.
  • 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.
  • 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.
  • HY-139346
    VX-150

    Sodium Channel Neurological Disease
    VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research.
  • HY-N6691
    Veratridine

    3-Veratroylveracevine

    Sodium Channel Neurological Disease
    Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
  • HY-110325
    PF-04885614

    Sodium Channel Neurological Disease
    PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment.
  • HY-12883A
    PF-05198007

    Sodium Channel Neurological Disease
    PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.
  • HY-19958
    XEN907

    Sodium Channel Neurological Disease
    XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.
  • HY-131182
    DS-1971a

    Sodium Channel Neurological Disease
    DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
  • HY-114237
    GDC-0276

    Sodium Channel Neurological Disease
    GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
  • 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.
  • HY-12883B
    PF 05089771 tosylate

    Sodium Channel Neurological Disease
    PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-12883
    PF 05089771

    Sodium Channel Neurological Disease
    PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-126005
    VGSC blocker-1

    Cancer
    VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability.
  • HY-126291
    GNE-616

    Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.
  • HY-P1441A
    Mambalgin 1 TFA

    Sodium Channel
    Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
  • HY-133012
    GFB-8438

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.