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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
10 Results for "
dorsal root ganglion cells
" in MedChemExpress (MCE) Product Catalog:
Products (10)
10 Results for "dorsal root ganglion cells" in MCE Product Catalog:
4
4 Cited Publications
Synonyms: YH25448; GNS-1480
Target:
Research Areas:
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 .
4
4 Cited Publications
Cat. No.: HY-N6789
CAS No.: 108068-98-0
Target:
Research Areas:
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 .
4
4 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 .
Cat. No.: HY-139201H
CAS No.: 27964-99-4
Synonyms: PDLHB (MW ≥300000)
Target:
Research Areas:
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 .
Cat. No.: HY-19858
CAS No.: 317844-33-0
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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 .
Cat. No.: HY-175340
CAS No.: 1361107-81-4
Target:
Research Areas:
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 .
Cat. No.: HY-130358
CAS No.: 179469-40-0
Target:
Research Areas:
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 .
Cat. No.: HY-187689
CAS No.: 1005056-10-9
RKN5755 is a β-arrestin1 inhibitor and a selective inhibitor of activated fibroblasts. RKN5755 binds to β-arrestin1 and interferes with the cofilin signaling pathway mediated by this protein to block its function. RKN5755 not only inhibits the enhanced migratory effect of fibroblasts co-cultured with cancer cells, but also prevents the inhibitory effect of EP3 agonists on the EP2 receptor-induced elevation of tetrodotoxin-resistant sodium currents in mouse dorsal root ganglion neurons. RKN5755 is widely used in research on related diseases such as cancer metastasis and pain .
Cat. No.: HY-109061A
CAS No.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
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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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
