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Results for "

NaV1 subtypes

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

7

Peptides

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16787
    ICA-121431
    4 Publications Verification

    		 Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
    ICA-121431
  • 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-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-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 .
    GFB-8438
  • 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-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-123414
    GX-936

    PF-05196233

    		 Sodium Channel Neurological Disease
    GX-936 (PF-05196233), a potent and Nav1.7-subtype selective inhibitor, binds to the activated state of voltage-sensor domain IV (VSD4) .
    GX-936
  • 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 .
    GNE-616
  • 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-P5811
    Ceratotoxin-1

    CcoTx1; β-TRTX-cm1a

    		 Sodium Channel Neurological Disease
    Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
    Ceratotoxin-1
  • HY-172903
    Nav1.8-IN-16

    		Sodium Channel Neurological Disease Inflammation/Immunology
    Nav1.8-IN-16 (Compound (R)-40) is an orally active and selective hNaV 1.8 inhibitor (IC50: 5.9 nM). Nav1.8-IN-16 exerts analgesic effects by blocking NaV1.8 channels without significantly affecting other NaV subtypes or hERG channels. Nav1.8-IN-16 exhibits dose-dependent analgesic effects in postoperative pain and inflammatory pain models and can be used in pain-related research .
    Nav1.8-IN-16
  • HY-P1219
    Jingzhaotoxin-III

    β-TRTX-Cj1α

    		 Sodium Channel Neurological Disease
    Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
    Jingzhaotoxin-III
  • 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 .
    Nav1.7-IN-8
  • HY-P5177
    GsAF-II

    		Sodium Channel Potassium Channel Neurological Disease
    GsAF-II is a peptide toxin that blocks hERG1 subtype potassium channels in a voltage-dependent manner. GsAF-II blocks Nav1.x subtype sodium channels .
    GsAF-II
  • HY-163855
    KGP-25

    		Sodium Channel GABA Receptor Neurological Disease
    KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia .
    KGP-25
  • HY-126005
    VGSC blocker-1

    		Sodium Channel 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 .
    VGSC blocker-1
  • HY-181063
    Nav1.5-IN-1

    		Sodium Channel Cardiovascular Disease
    Nav1.5-IN-1 is a selective Nav1.5 inhibitor with an IC50 of 1.38 μM. Nav1.5-IN-1 shows selectivity over other Nav subtypes. Nav1.5-IN-1 reduces cardiac conduction in isolated rat hearts.Nav1.5-IN-1 can be used for the research of arrhythmias .
    Nav1.5-IN-1
  • HY-183709
    Nav1.8-IN-24

    		Sodium Channel Neurological Disease
    Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
    Nav1.8-IN-24
  • HY-185334
    GNE-3565

    		Sodium Channel Neurological Disease
    GNE-3565 is an arylsulfonamide class NaV1.7 inhibitor with subnanomolar channel blockage and mixed subtype selectivity.GNE-3565 can be used for the research of pain .
    GNE-3565
  • HY-182334
    azo-Q2a

    		Sodium Channel Cardiovascular Disease
    azo-Q2a is a photoswitchable NaV1.5 inhibitor. azo-Q2a exists as the trans isomer with low activity in the dark or under 480 nm illumination, and exists as the cis isomer with higher inhibitory potency under 365 nm illumination. azo-Q2a reduces the heart rate of living zebrafish larvae in a light-dependent manner. azo-Q2a can be used for the study of arrhythmias .
    azo-Q2a

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