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Results for "

dorsal root ganglion neurons

" in MedChemExpress (MCE) Product Catalog:

39

Inhibitors & Agonists

1

Biochemical Assay Reagents

11

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N6825
    Hydroxy-α-sanshool
    3 Publications Verification

    		 TRP Channel Endogenous Metabolite Neurological Disease
    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 .
    Hydroxy-α-sanshool
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    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 .
    Lazertinib
  • HY-N6789
    KT5720
    4 Publications Verification

    		 PKA Neurological Disease Cancer
    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 .
    KT5720
  • HY-121119
    MRS 1523
    5 Publications Verification

    		 Adenosine Receptor Calcium Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    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 .
    MRS 1523
  • HY-120751
    TROX-1

    		Calcium Channel Neurological Disease
    TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
    TROX-1
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    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 .
    Lazertinib mesylate
  • HY-B1177
    Crotamiton

    		Environmental Pollutants TRP Channel Parasite Infection
    Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton
  • HY-W013712
    GI-530159

    		Potassium Channel Neurological Disease
    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 .
    GI-530159
  • HY-17355B
    Dexpramipexole
    2 Publications Verification

    (R)-Pramipexole; R-(+)-Pramipexole; KNS-760704

    		 PINK1/Parkin Glutathione Peroxidase Sodium Channel ATP Synthase NOD-like Receptor (NLR) Mitophagy Ferroptosis Autophagy Apoptosis Reactive Oxygen Species (ROS) Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Dexpramipexole ((R)-Pramipexole) is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more .
    Dexpramipexole
  • HY-W540972
    Primulin

    Primuline

    		 Fluorescent Dye HCV Dengue Virus Infection
    Primulin is a versatile fluorescent dye and bioactive compound widely used in analytical, biological, botanical and virological studies. Primulin acts as a versatile stain that labels plant cell walls and differentiates live and dead spermatozoa via distinct fluorescence patterns. Primulin exhibits strong albumin‑binding capacity. Primulin acts as a retrograde axonal tracer in neurobiological investigations. Primulin and its derivatives inhibit HCV NS3, block dengue virus NS3-mediated ATP hydrolysis, and disrupt HCV replicase assembly .
    Primulin
  • HY-P1604
    ATX-II
    1 Publications Verification

    		 Sodium Channel Cardiovascular Disease Inflammation/Immunology
    ATX-II is a selective sodium channel modulator toxin. ATX-II enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II has pro-arrhythmic effect. ATX-II slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome .
    ATX-II
  • HY-P1604A
    ATX-II TFA
    1 Publications Verification

    		 Sodium Channel Cardiovascular Disease Inflammation/Immunology
    ATX-II TFA is a selective sodium channel modulator toxin. ATX-II TFA enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II TFA has pro-arrhythmic effect. ATX-II TFA slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II TFA can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome .
    ATX-II TFA
  • HY-N6825R
    Hydroxy-α-sanshool (Standard)

    		Reference Standards TRP Channel Endogenous Metabolite Neurological Disease
    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 .
    Hydroxy-α-sanshool (Standard)
  • HY-P3071
    ShK toxin

    Stichodactyla helianthus neurotoxin

    		 Potassium Channel Neurological Disease Inflammation/Immunology
    ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
    ShK toxin
  • HY-168758
    Delta3,5-cholestadien-7-one

    		GABA Receptor Neurological Disease
    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 .
    Delta3,5-cholestadien-7-one
  • HY-P2707
    α-Dendrotoxin

    α-DTX

    		 Sodium Channel Potassium Channel Neurological Disease
    α-Dendrotoxin (α-DTX) is a voltage-gated K + channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks Kv1.1, Kv1.2, Kv1.6 and D-type (ID) voltage-gated K + channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures .
    α-Dendrotoxin
  • HY-P10358
    TAT-CBD3A6K

    		Calcium Channel Neurological Disease
    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 .
    TAT-CBD3A6K
  • HY-155017
    6-Iodoamiloride

    		Sodium Channel Neurological Disease Cancer
    6-Iodoamiloride is a potent acid-sensing ion channel 1 (ASIC1) inhibitor with an IC50 of 88 nM. 6-Iodoamiloride inhibits ASIC3-mediated currents from rat dorsal root ganglion neurons with an IC50 of 230 nM .
    6-Iodoamiloride
  • HY-19858
    LY-466195

    		iGluR Neurological Disease
    LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
    LY-466195
  • HY-P3071A
    ShK toxin TFA

    Stichodactyla helianthus neurotoxin TFA

    		 Potassium Channel Neurological Disease Inflammation/Immunology
    ShK toxin TFA (Stichodactyla helianthus neurotoxin TFA) is a neurotoxin. ShK toxin TFA blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin TFA can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin TFA competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin TFA suppresses K + currents in cultured rat dorsal root ganglion neurons. ShK toxin TFA also inhibits T lymphocyte proliferation .
    ShK toxin TFA
  • HY-175340
    Kv7.2/Kv7.3 activator-3

    		Potassium Channel TSPO Neurological Disease
    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 .
    Kv7.2/Kv7.3 activator-3
  • HY-130358
    PDDHV

    		Calcium Channel Neurological Disease
    PDDHV is a calcium absorption inducer and may achieve 45Ca 2+ influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
    PDDHV
  • HY-P5180
    Hainantoxin-III

    		Sodium Channel Neurological Disease
    Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
    Hainantoxin-III
  • HY-P5773
    Jingzhaotoxin-34

    		Sodium Channel Neurological Disease
    Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC50 of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons .
    Jingzhaotoxin-34
  • HY-P5868
    mHuwentoxin-IV

    		Sodium Channel Neurological Disease
    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 .
    mHuwentoxin-IV
  • HY-121122
    A778317

    		TRP Channel Others
    A778317 is a TRPV1 antagonists. A778317 can block changes in intracellular calcium levels mediated by TRPV1 receptors, with a pIC50 value of 8.31. A-778317 can also block the activation of natural rat TRPV1 receptors in dorsal root ganglion neurons by capsaicin and acid .
    A778317
  • HY-P5770
    Jingzhaotoxin-V

    		Sodium Channel Neurological Disease
    Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC50 of 604.2 nM) .
    Jingzhaotoxin-V
  • HY-108576
    Linopirdine dihydrochloride

    DuP 996 dihydrochloride

    		 TRP Channel Neurological Disease
    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 .
    Linopirdine dihydrochloride
  • HY-P10358A
    TAT-CBD3A6K acetate

    		Calcium Channel Neurological Disease
    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 .
    TAT-CBD3A6K acetate
  • HY-121119R
    MRS 1523 (Standard)

    		Adenosine Receptor Calcium Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    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 .
    MRS 1523 (Standard)
  • HY-B1177R
    Crotamiton (Standard)

    		Reference Standards Parasite TRP Channel Infection
    Crotamiton (Standard) is the analytical standard of Crotamiton. This product is intended for research and analytical applications. Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton (Standard)
  • HY-108459
    6-Iodonordihydrocapsaicin

    		TRP Channel Neurological Disease
    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 .
    6-Iodonordihydrocapsaicin
  • HY-182500A
    (S,S)-SARM1-IN-9

    		Toll-like Receptor (TLR) Neurological Disease
    (S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1 C311A or SARM1 C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy .
    (S,S)-SARM1-IN-9
  • HY-185007
    LI-633

    		GABA Receptor Neurological Disease
    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 .
    LI-633
  • HY-120751A
    (S)-TROX-1

    		Drug Isomer Calcium Channel Neurological Disease
    (S)-TROX-1 is the S-enantiomer of TROX-1 (HY-120751). TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
    (S)-TROX-1
  • HY-182710
    DA-0218

    		Sodium Channel Neurological Disease
    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 .
    DA-0218
  • HY-165459
    KJM429

    MK-056

    		 TRP Channel Infection Inflammation/Immunology
    KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
    KJM429
  • HY-182500
    SARM1-IN-9

    		Toll-like Receptor (TLR) Neurological Disease
    SARM1-IN-9 (Compound MY-13B) is a stereoselective SARM1 inhibitor. SARM1-IN-9 is applicable to research related to axon degeneration-dependent neurological diseases .
    SARM1-IN-9
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    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 .
    Lazertinib mesylate hydrate

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