2. シグナル伝達
  3. Membrane Transporter/Ion Channel
  4. Sodium Channel
  5. Nav1.7 Isoform

Nav1.7

NaV1.7, encoded by SCN9A, is a voltage-gated sodium channel strongly linked to human nociception, because loss-of-function mutations cause congenital inability to experience pain[1]. Mechanistically, NaV1.7 supports nociceptor excitability and pain signaling, and human studies show that NaV1.7 loss can produce a profound loss of functional nociceptors[2]. In disease models and inherited pain syndromes, gain-of-function SCN9A mutations are associated with paroxysmal extreme pain disorder and related painful phenotypes[3]. Compared with related isoforms, human dorsal root ganglion neurons show higher NaV1.7 expression and lower NaV1.8 expression than mouse dorsal root ganglion neurons, which is relevant for translational pain research[4]. For experimental applications, inflammatory mediators such as NGF and IL-6 sensitize adult dorsal root ganglion neurons, and combined NaV1.7/NaV1.8 blockade strongly affects thermally evoked firing[5]. Structural studies of NaV1.7 antagonists map drug-binding sites and support rational inhibitor design[6].

Nav1.7 関連製品 (58):

製品番号 製品名 製品効果 純度
  • HY-N1847
    3'-Methoxydaidzein Inhibitor 99.67%
    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.
  • HY-101789
    Nav1.7-IN-3 Inhibitor 98.21%
    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-119934
    NaV1.7 inhibitor-1 Inhibitor 99.17%
    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-122001
    PF-05186462 Inhibitor 99.69%
    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-P1220A
    Huwentoxin-IV TFA Inhibitor 99.18%
    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-123825
    GX-674 Antagonist 98.45%
    GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV.
  • HY-12883A
    PF-05198007 Inhibitor 99.27%
    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-146069
    ABBV-318 Inhibitor 98.72%
    ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain.
  • HY-178281
    E0199 Inhibitor 99.89%
    E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research.
  • HY-156596
    Aneratrigine Inhibitor 99.60%
    Aneratrigine is a selective Nav1.7 inhibitor with an IC50 of 19 nM. Aneratrigine is applicable for pain-related research.
  • HY-P1681A
    GpTx-1 TFA Antagonist 99.56%
    GpTx-1 TFA is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.
  • HY-P1073
    ProTx-I Inhibitor
    ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.
  • HY-178494
    Nav1.7-IN-19 Inhibitor 98.87%
    Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC50 of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease.
  • HY-108425B
    (Rac)-AMG8379 Antagonist 99.25%
    (Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
  • HY-16723A
    (R)-Funapide Inhibitor 99.22%
    (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.
  • HY-15736
    Sodium Channel inhibitor 1 Inhibitor 99.38%
    Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50 of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain.
  • HY-P1221
    ProTx II Inhibitor 98.34%
    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-19366
    Nav1.7-IN-2 Inhibitor 98.28%
    Nav1.
  • HY-102998
    Nav1.7-IN-6 Inhibitor
    Nav1.7-IN-6 (example 346) is a Nav1.7 selective inhibitor, which is extracted from patent WO2015078374A1.
  • HY-126291
    GNE-616 Inhibitor
    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.