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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
DRG neuron
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "DRG neuron" in MCE Product Catalog:
10
10 Publications Verification
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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 .
5
5 Cited Publications
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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 .
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4
4 Cited Publications
Cat. No.: HY-N6789
CAS No.: 108068-98-0
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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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4 Cited Publications
Synonyms: EMA401; PD-126055; (S)-EMA400
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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 .
3
3 Cited Publications
Cat. No.: HY-N6825
CAS No.: 83883-10-7
Category:
Zanthoxylum bungeanum Maxim. Alkaloids Other Alkaloids Rutaceae Plants Endogenous metabolite
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3
3 Cited Publications
Synonyms: YH25448; GNS-1480
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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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3 Cited Publications
Cat. No.: HY-109061B
CAS No.: 2247995-37-3
Synonyms: YH25448 mesylate; GNS-1480 mesylate
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 .
2
2 Cited Publications
Synonyms: WS-12; AR-15512; AVX-012
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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 .
Synonyms: 4αPDD
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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) .
Cat. No.: HY-N2500
CAS No.: 19186-35-7
Category:
Cardiovascular Disease Infection other families Centaurea ornata Lignans Phenylpropanoids Plants Umbelliferae Disease Research Fields
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ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM .
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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 .
Cat. No.: HY-164795A
CAS No.: 2772746-58-2
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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 .
Cat. No.: HY-164795
CAS No.: 1849603-79-7
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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 .
Cat. No.: HY-W013712
CAS No.: 69563-88-8
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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 .
Cat. No.: HY-N5060S
CAS No.: 1335401-40-5
Synonyms: 4-Allylanisole-d4
Cat. No.: HY-101546A
CAS No.: 32728-75-9
Synonyms: (+)-Cavidine
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Cat. No.: HY-111560
CAS No.: 1956337-58-8
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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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
