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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
9 Results for "
orthosteric agonist activity
" in MedChemExpress (MCE) Product Catalog:
Products (9)
9 Results for "orthosteric agonist activity" in MCE Product Catalog:
1
1 Cited Publications
Cat. No.: HY-W011417
CAS No.: 606-59-7
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Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
Cat. No.: HY-W011417R
CAS No.: 606-59-7
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Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
Cat. No.: HY-117764
CAS No.: 1413405-33-0
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LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
Cat. No.: HY-135698
CAS No.: 117339-76-1
Synonyms: M-CAM
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Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .
Cat. No.: HY-182729
CAS No.: 1229363-11-4
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FFA2 agonist-2 is a potent agonist of the FFA2 (GPR43) receptor, with a pEC50 of 7.9 for human FFA2, and a pEC50 of 7.3 for murine FFA2. FFA2 agonist-2 acts as an orthosteric agonist and shows no obvious cross‑activity against FFA1, FFA3 and FFA4. FFA2 agonist-2 can be used for FFA2 receptor research in type 2 diabetes and metabolic disorders .
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Cat. No.: HY-187504
CAS No.: 3129083-72-0
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5-HT2A receptor activator-1 is an allosteric modulator of the 5-HT2A receptor, with an EC50 of 0.56 μM. 5-HT2A receptor activator-1 exerts allosteric interaction with the 5-HT2A receptor, enhances 5-HT-induced receptor activation by binding to the allosteric site, and shows no obvious agonistic activity on its own. 5-HT2A receptor activator-1 can be used in the research of neurological or psychiatric disorders .
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VUF-6884 (Compound 7j) is a histamine receptor (Histamine Receptor) ligand with activity toward human H4R and H1R. Its pEC50 and pKi values against human H4R are 7.70 and 7.55, respectively, while those against human H1R are 8.17 and 8.11, respectively. VUF-6884 competitively binds to the orthosteric binding site of human H4R to displace histamine, and exhibits inverse agonist activity at human H1R .
Cat. No.: HY-187560
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VCU-1012 is a serotonin 2A receptor (5-HT2AR) agonist, with a pEC50 of 5.81 and a pKi of 5.75 against human receptors. VCU-1012 binds to the canonical orthosteric binding pocket of 5-HT2AR, triggers intracellular calcium release and Gαq protein dissociation, and its agonistic activity depends on specific amino acid residues in the receptor binding pocket. VCU-1012 can be used in research related to depression, anxiety disorders, and chemotherapy-induced mood disorders .
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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
