Search Result
Results for "
DRG
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N6691
-
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3-Veratroylveracevine
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Sodium Channel
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Neurological Disease
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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 .
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- HY-N6825
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- HY-109061
-
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YH25448; GNS-1480
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Apoptosis
Akt
TRP Channel
EGFR
ERK
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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- HY-108449
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WS-12; AR-15512; AVX-012
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TRP Channel
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Neurological Disease
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Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
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- HY-118122
-
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FIAU; DRG-0098; NSC 678514
|
HSV
HBV
DNA/RNA Synthesis
Orthopoxvirus
Nucleoside Antimetabolite/Analog
|
Infection
|
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Fialuridine (FIAU), a nucleoside analog, is a HSV-1 and HSV-2 inhibitor with Kis of 0.14 μM and 0.95 μM, respectively. Fialuridine shows anti-orthopoxvirus and anti-hepatitis B virus (HBV) activities. Fialuridine inhibits duck HBV DNA replication with IC50 values of 0.075 μM and 156 μM in human hepatoma cells and in chicken liver cells, respectively .
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- HY-N6789
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KT5720
4 Publications Verification
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PKA
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Neurological Disease
Cancer
|
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KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
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- HY-116291
-
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4αPDD
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TRP Channel
CHIKV
|
Infection
Inflammation/Immunology
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4α-Phorbol 12,13-didecanoate (4αPDD) is a transient receptor potential vanilloid 4 (TRPV4) agonist. 4α-Phorbol 12,13-didecanoate can promote Ca 2+ influx, induce ATP release and function as an osmoreceptor. 4α-Phorbol 12,13-didecanoate can inhibit water intake and increase maximal micturition pressure in rats. 4α-Phorbol 12,13-didecanoate can be used for the researches of inflammation and infection, such as chikungunya virus (CHIKV) .
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- HY-101160
-
|
DRG16
|
DNA Alkylator/Crosslinker
ADC Payload
|
Cancer
|
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SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent .
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- HY-13106
-
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EMA401; PD-126055; (S)-EMA400
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Angiotensin Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
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Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
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- HY-121119
-
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Adenosine Receptor
Calcium Channel
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .
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- HY-N5060
-
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4-Allylanisole
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Environmental Pollutants
Parasite
Apoptosis
Keap1-Nrf2
NF-κB
|
Infection
Neurological Disease
Inflammation/Immunology
|
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Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity .
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- HY-110150
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UNC3230
Maximum Cited Publications
9 Publications Verification
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PI4P5K
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Neurological Disease
Inflammation/Immunology
Cancer
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UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
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- HY-114332
-
|
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MAP3K
JNK
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Neurological Disease
Metabolic Disease
|
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GNE-8505 is an orally active, blood-brain barrier-permeable selective dual leucine zipper kinase (DLK) inhibitor. GNE-8505 has an IC50 of 0.144 μM for pJNK, and EC50 of 0.457 μM for DRG. GNE-8505 inhibits the DLK/JNK pathway, reduces stress-induced c-Jun phosphorylation levels, decreases neuronal death and suppresses axonal degeneration. GNE-8505 reduces phosphorylated c-Jun levels in the retina, spinal cord and brain tissues of mice. GNE-8505 is applicable to research related to Alzheimer's disease and amyotrophic lateral sclerosis (ALS) .
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- HY-109061B
-
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YH25448 mesylate; GNS-1480 mesylate
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TRP Channel
EGFR
Akt
ERK
Apoptosis
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Cancer
|
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Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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- HY-N2500
-
|
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Microtubule/Tubulin
Apoptosis
Autophagy
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Infection
Cardiovascular Disease
Cancer
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Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from Anthriscus sylvestris. Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis . Deoxypodophyllotoxin induces cell autophagy and apoptosis . Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons .
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- HY-110285
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-
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- HY-157802
-
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Sodium Channel
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Neurological Disease
|
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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 .
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- HY-124619
-
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EAAT
HIV
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Neurological Disease
|
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GPI-1046 is an orally active, antibiotic-free immunophilin ligand that reduces ethanol intake by upregulating glutamate transporter 1 (GLT1) in the prefrontal cortex (PFC) and nucleus accumbens core (NAc-core). GPI-1046 improves human immunodeficiency virus (HIV)-associated sensory neuropathy (HIV-SN) by attenuating store-operated calcium (SOC) entry. GPI-1046 has neuroprotective activity .
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- HY-164795A
-
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
|
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SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
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- HY-164795
-
|
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
|
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SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
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- HY-W013712
-
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Potassium Channel
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Neurological Disease
|
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GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
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- HY-118941
-
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Prostaglandin Receptor
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Cardiovascular Disease
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BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure .
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- HY-N5060S
-
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4-Allylanisole-d4
|
Parasite
Isotope-Labeled Compounds
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Neurological Disease
|
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Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [10] .
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- HY-101546A
-
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(+)-Cavidine
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p38 MAPK
ERK
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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Cavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain .
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- HY-126789
-
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Biochemical Assay Reagents
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Metabolic Disease
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DM-Nitrophen is a photolabile caged calcium compound that acts as a calcium releaser. DM-Nitrophen binds Ca 2+ with high affinity and Mg 2+ with considerable affinity before photolysis. DM-Nitrophen releases Ca 2+ into the cytosol upon ultraviolet light irradiation. DM-Nitrophen induces calcium concentration pulses, triggers cytosolic calcium transients, promotes calcium-dependent exocytosis. DM-Nitrophen can be used for the research of calcium-dependent cellular processes .
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- HY-12761
-
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Cannabinoid Receptor
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Cardiovascular Disease
Others
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc .
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- HY-111560
-
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Potassium Channel
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Neurological Disease
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IQM-266 is a Downstream Regulatory Element Antagonist Modulator (DREAM) ligand with a KD of 4.63 μM. IQM-266 inhibits the KV4.3/DREAM current in a concentration-, voltage-, and time-dependent-manner. IQM-266 also modulates A-type outward potassium currents (IA) from rat dorsal root ganglia (DRG) neurons. IQM-266 can be used for neurological disease research, such as Alzheimer’s disease and Huntington's disease (HD) .
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- HY-108425
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Sodium Channel
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Neurological Disease
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AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
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- HY-N6825R
-
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Reference Standards
TRP Channel
Endogenous Metabolite
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Neurological Disease
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Hydroxy-α-sanshool (Standard) is the analytical standard of Hydroxy-α-sanshool. This product is intended for research and analytical applications. Hydroxy-α-sanshool is a transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50s of 69 and 1.1 μM, respectively. Hydroxy-α-sanshool can be used for pain research .
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- HY-168758
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GABA Receptor
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Neurological Disease
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Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
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- HY-N14827
-
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SM-216289
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Drug Derivative
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Neurological Disease
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Xanthofulvin (SM-216289) is an inhibitor of semaphorin 3A. Xanthofulvin blocks its binding to receptors, inhibits growth cone collapse, and accelerates olfactory nerve regeneration in rats in vivo. Xanthofulvin can be used in studies related to traumatic neuronal injury .
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- HY-P10358
-
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Calcium Channel
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Neurological Disease
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TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-13106A
-
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EMA401 sodium; PD-126055 sodium
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Angiotensin Receptor
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Neurological Disease
Endocrinology
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Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
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- HY-157802A
-
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Sodium Channel
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Neurological Disease
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(S)-LTGO-33 is a small molecule inhibitor of voltage-gated sodium channel NaV1.8. (S)-LTGO-33 can be used in the study of pain disorders .
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- HY-P5756
-
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Opioid Receptor
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Neurological Disease
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CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
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- HY-12914
-
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain .
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- HY-N6691R
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3-Veratroylveracevine (Standard)
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Reference Standards
Sodium Channel
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Neurological Disease
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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 .
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- HY-171778
-
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
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QLS-81 is a Nav1.7 channel inhibitor (IC50: 1.5 μM). QLS-81 has significant analgesic activity and can relieve neuropathic and inflammatory pain. QLS-81 exerts frequency-dependent inhibitory effects by inhibiting the inactivated state of Nav1.7 channels. QLS-81 can be used in the study of chronic pain .
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- HY-172903
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-175340
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Potassium Channel
TSPO
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Neurological Disease
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Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
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- HY-RS18925
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Small Interfering RNA (siRNA)
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Others
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Drg1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Drg1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Drg1 Mouse Pre-designed siRNA Set A
Drg1 Mouse Pre-designed siRNA Set A
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- HY-RS04010
-
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Small Interfering RNA (siRNA)
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Others
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DRG2 Human Pre-designed siRNA Set A contains three designed siRNAs for DRG2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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DRG2 Human Pre-designed siRNA Set A
DRG2 Human Pre-designed siRNA Set A
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- HY-RS04009
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Small Interfering RNA (siRNA)
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Others
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DRG1 Human Pre-designed siRNA Set A contains three designed siRNAs for DRG1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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DRG1 Human Pre-designed siRNA Set A
DRG1 Human Pre-designed siRNA Set A
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- HY-161327
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HBV
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Infection
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HBV-IN-44 (Compound (S)-2a) is a HBV inhibitor with a IC50 value of 23 nM for HbsAg. HBV-IN-44 is less toxic to the neurite growth of HT22 cells and DRG neurons in vitro .
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- HY-P10358A
-
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Calcium Channel
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Neurological Disease
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TAT-CBD3A6K acetate, is a modified TAT-CBD3 peptide. TAT-CBD3A6K acetate reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K acetate shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-116704
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-
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- HY-P5868
-
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Sodium Channel
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Neurological Disease
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mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC50 of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages .
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- HY-162347
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Sodium Channel
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Neurological Disease
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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 .
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- HY-121119R
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Adenosine Receptor
Calcium Channel
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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MRS 1523 (Standard) is the analytical standard of MRS 1523. This product is intended for research and analytical applications. MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .
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- HY-108576
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DuP 996 dihydrochloride
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TRP Channel
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Neurological Disease
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Linopirdine dihydrochloride is a agonist of capsaicin receptor TRPV1. Linopirdine increases the intracellular calcium concentration in HEK293 cells. Linopirdine dihydrochloride exerts an excitatory action on mammalian nociceptors .
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- HY-P5782
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Sodium Channel
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Neurological Disease
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δ-Theraphotoxin-Hm1a toxin is a selective Nav1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome .
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- HY-RS25415
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Small Interfering RNA (siRNA)
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Others
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Drg1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Drg1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Drg1 Rat Pre-designed siRNA Set A
Drg1 Rat Pre-designed siRNA Set A
- HY-101160R
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DRG16 (Standard)
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DNA Alkylator/Crosslinker
Reference Standards
ADC Payload
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Cancer
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SG2057 (Standard) is the analytical standard of SG2057 (HY-101160). This product is intended for research and analytical applications. SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent .
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- HY-179523
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Drug Derivative
NAMPT
Microtubule/Tubulin
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Neurological Disease
Cancer
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Carba1 is a bifunctional Carbazole (HY-D0204) derivative that activates nicotinamide phosphoribosyltransferase (NAMPT) and enhances NAD biosynthesis. Carba1 binds to colchicine site of tubulin, enhancing the anti-tumor effect of various chemotherapy drugs, such as Paclitaxel (HY-B0015). Carba1 exerts neuroprotective effect and can regulate cell energy metabolism. Carba1 can be used for the researches of cancer and chemotherapy-induced peripheral neuropathy (CIPN) .
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- HY-185007
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GABA Receptor
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Neurological Disease
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LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC50 of 70.4 nM. LI-633 can be used for the study of visceral pain .
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- HY-110268
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CXCR
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Inflammation/Immunology
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NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
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- HY-108449R
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WS-12 (Standard); AR-15512 (Standard); AVX-012 (Standard)
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Reference Standards
TRP Channel
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Neurological Disease
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Acoltremon (Standard) is the analytical standard of Acoltremon (HY-108449). This product is intended for research and analytical applications. Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
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- HY-182940
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Toll-like Receptor (TLR)
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Neurological Disease
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SARM1-IN-10 is an orally active SARM1 inhibitor with a pIC50 of 7.1 and a pKd of 8.3. As a base-exchange inhibitor, SARM1-IN-10 forms a NAD + adduct at the active site of the TIR domain of SARM1, blocks enzymatic function, and induces a unique rotameric state of W662 at the catalytic site of SARM1. SARM1-IN-10 acts as a paradoxical neurodegeneration inducer at low doses and an inhibitor at high doses, and it can exacerbate or protect against SARM1-mediated neurodegeneration depending on concentration. SARM1-IN-10 can be used in studies of peripheral neurodegeneration .
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- HY-109061BR
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YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
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Reference Standards
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Cancer
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Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
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- HY-N12768
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MDM-2/p53
Notch
Calcium Channel
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Neurological Disease
Inflammation/Immunology
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Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. Don (Ericaceae) (RM). Rhodojaponin VI binds rat N-Ethylmaleimide-sensitive fusion (NSF) with a Kd of 1.03 μM. Rhodojaponin VI blocks the MDM2-Notch1 signalling pathway by reducing MDM2 and Notch1 expression. Rhodojaponin VI indirectly reduces Cav2.2 current intensity by inhibiting NSF-mediated Cav2.2 trafficking. Rhodojaponin VI alleviates glomerulonephritis progression and podocyte injury in passive heymann nephritis rats. Rhodojaponin VI also has antinociceptive effects. Rhodojaponin VI can be used for the researches of heymann nephritis and pain .
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- HY-181662
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MAP3K
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Neurological Disease
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DLK-IN-2 is a selective inhibitor of DLK and neuroprotective agent. DLK-IN-2 shows no significant inhibition against CYPs 3A4, 2D6 and 2C9. DLK-IN-2 inhibits acute axonal palmitoylation of DLK, blocks DLK-dependent pro-degenerative axon-to-soma retrograde signaling and suppresses c-Jun phosphorylation. DLK-IN-2 can be used for the mechanistic study of neurodegenerative diseases .
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- HY-109061A
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YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
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Apoptosis
Akt
TRP Channel
EGFR
ERK
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Cancer
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Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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- HY-182710
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Sodium Channel
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Neurological Disease
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DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus .
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- HY-108459
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TRP Channel
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Neurological Disease
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6-Iodonordihydrocapsaicin is a TRPV1 antagonist. 6-Iodonordihydrocapsaicin functionally blocks TRPV1-mediated responses, including capsaicin-induced ion currents in dorsal root ganglion neurons and distension-induced firing of jejunal spinal afferent fibers in mice. 6-Iodonordihydrocapsaicin can be used in the research of visceral pain and anxiety disorders .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10358
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Calcium Channel
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Neurological Disease
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TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-P5756
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Opioid Receptor
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Neurological Disease
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CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
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- HY-P10358A
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Calcium Channel
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Neurological Disease
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TAT-CBD3A6K acetate, is a modified TAT-CBD3 peptide. TAT-CBD3A6K acetate reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K acetate shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-P5868
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Sodium Channel
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Neurological Disease
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mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC50 of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages .
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- HY-P5782
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Sodium Channel
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Neurological Disease
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δ-Theraphotoxin-Hm1a toxin is a selective Nav1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome .
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* This product has been "discontinued".
Optimized version of product available:
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Product Name |
Chemical Structure |
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- HY-N5060S
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Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [10] .
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- HY-RS18925
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siRNAs
Mouse Pre-designed siRNA Sets
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Drg1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Drg1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS04010
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siRNAs
Human Pre-designed siRNA Sets
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DRG2 Human Pre-designed siRNA Set A contains three designed siRNAs for DRG2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS04009
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siRNAs
Human Pre-designed siRNA Sets
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DRG1 Human Pre-designed siRNA Set A contains three designed siRNAs for DRG1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS25415
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siRNAs
Rat Pre-designed siRNA Sets
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Drg1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Drg1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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