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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
75 Results for "
calcium response
" in MedChemExpress (MCE) Product Catalog:
Products (75)
75 Results for "calcium response" in MCE Product Catalog:
13
13 Publications Verification
Synonyms: AZD9668
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Alvelestat (AZD9668) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis .
4
4 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 .
4
Category:
Cardiovascular Disease Flavonols Flavonoids Phenols Polyphenols Plants Other Families Extract Disease Research Fields
Target:
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 .
1
1 Cited Publications
Cat. No.: HY-D0976
CAS No.: 202983-32-2
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Research Areas:
NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC50 value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection .
1
1 Cited Publications
Cat. No.: HY-N6850
CAS No.: 26020-14-4
1
1 Cited Publications
Cat. No.: HY-N0805A
CAS No.: 18649-93-9
Category:
Triterpenes Alisma plantago-aquatica Linn. Terpenoids Metabolic Disease Plants Disease Research Fields Alismataceae Extract
Target:
1
1 Cited Publications
Cat. No.: HY-172241
CAS No.: 1436920-57-8
Synonyms: RZL-012; Utenpanium chloride
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Research Areas:
Tapencarium (RZL-012; Utenpanium chloride) is an injectable fat volume-reducing agent. Tapencarium irreversibly impairs cell membrane integrity, increases membrane permeability, induces elevated cytoplasmic calcium, alters mitochondrial membrane potential, and triggers necrosis. Tapencarium induces fat necrosis, inflammatory responses and fibrous tissue formation at the injection site. Tapencarium can be used in research related to submental fat excess and Dercum's disease .
1
1 Cited Publications
Cat. No.: HY-P85890
Synonyms: AIF 1; AIF-1; Aif1; AIF1 protein; AIF1_HUMAN; Allograft inflammatory factor 1; Allograft inflammatory factor 1 splice variant G; allograft inflammatory factor-1 splice variant Hara-1; balloon angioplasty responsive transcription; BART 1; G1; G1 putative splice variant of allograft inflamatory factor 1; IBA 1; IBA1; interferon gamma responsive transcript; Interferon responsive transcript 1; interferon responsive transcript factor 1; Ionized calcium binding adapter molecule 1; Ionized calcium-binding adapter molecule 1; ionized calcium-binding adapter molecule; IRT 1; IRT1; Microglia response factor; MRF1; Protein g1;
Cat. No.: HY-P10408
CAS No.: 1906866-53-2
Research Areas:
Cat. No.: HY-153468
CAS No.: 3035547-78-2
Synonyms: TEQ103; Sera2
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Research Areas:
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of histamine H1 receptor and TRPV1 receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms .
Synonyms: NCGC84
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Research Areas:
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
Cat. No.: HY-P1636
CAS No.: 113274-56-9
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Research Areas:
Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
Cat. No.: HY-W145486
CAS No.: 299-28-5
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YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively .
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trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis .
Cat. No.: HY-19664
CAS No.: 99522-79-9
Synonyms: OPC-13340
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Research Areas:
Pranidipine (OPC-13340) is an orally active L-type voltage-dependent calcium channel (L-VDCC) blocker with a Ki value of 0.16 nM. Pranidipine inhibits calcium-induced contraction, suppresses slow-response action potentials, shortens action potential duration, reduces systolic and diastolic blood pressure, and exerts vasodilatory effects. Pranidipine enhances its vasodilatory effect by blocking NO decomposition. Pranidipine can be used in research related to essential hypertension, angina pectoris, myocardial infarction, and dilated cardiomyopathy .
Synonyms: SCH-10304
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Research Areas:
Clonixin (SCH-10304) is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca 2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain .
Cat. No.: HY-177873
CAS No.: 620940-01-4
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Research Areas:
AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC50 = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia .
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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
