6

MRS 1523

6 Publications Verification

Cat. No.: HY-121119

CAS No.: 212329-37-8

Purity: 99.97%

Target:

Adenosine Receptor Calcium Channel

Research Areas:

Cardiovascular Disease Neurological Disease Inflammation/Immunology

MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i 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 A_2A 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

Lazertinib

4 Cited Publications

Cat. No.: HY-109061

CAS No.: 1903008-80-9

Purity: 99.87%

Synonyms: YH25448; GNS-1480

Target:

Apoptosis Akt TRP Channel EGFR ERK

Research Areas:

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 .

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4

KT5720

4 Cited Publications

Cat. No.: HY-N6789

CAS No.: 108068-98-0

Target:

PKA

Research Areas:

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 .

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4

Olodanrigan

4 Cited Publications

Cat. No.: HY-13106

CAS No.: 1316755-16-4

Purity: 98.89%

Synonyms: EMA401; PD-126055; (S)-EMA400

Target:

Angiotensin Receptor

Research Areas:

Cardiovascular Disease Neurological Disease Endocrinology

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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4

Lazertinib mesylate

4 Cited Publications

Cat. No.: HY-109061B

CAS No.: 2247995-37-3

Synonyms: YH25448 mesylate; GNS-1480 mesylate

Target:

TRP Channel EGFR Akt ERK Apoptosis

Research Areas:

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 .

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1

H-20

1 Cited Publications

Cat. No.: HY-P10908

CAS No.: 3020015-02-2

Target:

PD-1/PD-L1 Opioid Receptor

Research Areas:

Neurological Disease

H-20 is a PD-1 agonist peptide. H-20 increases μOR mRNA in DRG neurons and modulates μOR-mediated analgesia. H-20 produces synergistic analgesic effects in inflammatory pain models and can reduce analgesic-induced tolerance, hyperalgesia, constipation, and motor impairment. H-20 can be used in pain-related research .

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