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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
57 Results for "
membrane binding sites
" in MedChemExpress (MCE) Product Catalog:
Products (57)
57 Results for "membrane binding sites" in MCE Product Catalog:
49
49 Publications Verification
Synonyms: MK-801
Target:
Research Areas:
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
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N-1-Naphthylphthalamic acid (Alanap 1) is a modulator of polar auxin transport that competes with auxin (indole-3-acetic acid, IAA) for membrane binding sites. N-1-Naphthylphthalamic acid also disrupts maize leaf initiation, KNOX protein regulation, and leaf margin formation .
3
3 Cited Publications
Synonyms: YH25448; GNS-1480
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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 .
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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 .
1
1 Cited Publications
Target:
Research Areas:
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
1
1 Cited Publications
Synonyms: ANSA; 8-Anilino-1-naphthalenesulfonic acid
1
1 Cited Publications
Cat. No.: HY-D1605
CAS No.: 1180490-57-6
1
1 Cited Publications
Research Areas:
EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
Cat. No.: HY-164036
CAS No.: 2930690-12-1
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Lolamicin is an orally effective inhibitor that specifically targets the Gram-negative bacteria lipoprotein transport system LolCDE complex. It selectively inhibits the transmembrane transport of outer membrane lipoproteins by competitively binding to lipoprotein binding sites. Lolamicin destroys the integrity of the bacterial outer membrane, leading to cell death, and has both bactericidal and antibacterial activity. It has significant effects on multidrug-resistant Enterobacteriaceae pathogens (such as Escherichia coli and Klebsiella pneumoniae). Lolamicin can be used to inhibit the study of acute pneumonia, sepsis and other infections caused by Gram-negative bacteria .
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Hyaluronic acid sodium (MW 200-1560) is a biopolymer composed of repeating disaccharide units, with a molecular weight of 200-1560. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid sodium exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid sodium activates PI3K-Akt signaling. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid sodium is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid sodium can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid sodium can lubricate the corneal endothelium. Hyaluronic acid sodium can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid sodium has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid sodium can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
Synonyms: Hyaluronan, low endotoxin; Hyaluronate, low endotoxin
Cat. No.: HY-18698
CAS No.: 142326-59-8
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Research Areas:
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
Cat. No.: HY-NP180
Synonyms: Lu-135252
Target:
Research Areas:
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
Cat. No.: HY-N9279
CAS No.: 23291-96-5
Synonyms: Monocrotaline pyrrole; MCTP; 3,8-Didehydromonocrotaline
Target:
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitory activity of C450-0730 against LuxN I209F was not significant .
Cat. No.: HY-116425R
CAS No.: 132-66-1
Synonyms: Alanap 1 (Standard)
Target:
Research Areas:
N-1-Naphthylphthalamic acid (Standard) is the analytical standard of N-1-Naphthylphthalamic acid. This product is intended for research and analytical applications. N-1-Naphthylphthalamic acid (Alanap 1) is a modulator of polar auxin transport that competes with auxin (indole-3-acetic acid, IAA) for membrane binding sites. N-1-Naphthylphthalamic acid also disrupts maize leaf initiation, KNOX protein regulation, and leaf margin formation .
Synonyms: L-Dihydroalprenolol
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(-)-Dihydroalprenolol (L-Dihydroalprenolol) is a β-adrenergic antagonist that inhibits the activity of β-adrenergic receptors. (-)-Dihydroalprenolol can cause desensitization of approximately 60% of β-adrenergic receptor binding sites. (-)-Dihydroalprenolol has also been shown to reduce the binding capacity of specific β-adrenergic ligands. (-)-Dihydroalprenolol may affect the ability to stimulate membrane-bound adenylate acylase .
Cat. No.: HY-19578B
CAS No.: 874882-92-5
Synonyms: (±)-Isamoltane hemifumarate
Target:
Research Areas:
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity .
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8-Aminoadenine is an adenine receptor 1 (rAde1R) inhibitor with a Ki of 6.51 μM in rat and 0.0341 μM in human. 8-Aminoadenine inhibits isoprenaline-induced cAMP accumulation and adenine uptake in astrocytoma cells expressing rAde1R. 8-Aminoadenine serves as a lead structure for the development of adenine receptor ligands to elucidate the functions of the adenine receptor family .
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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
