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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
36 Results for "
orthosteric agonist
" in MedChemExpress (MCE) Product Catalog:
Products (36)
36 Results for "orthosteric agonist" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: AVL-3288; UCI-4083
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CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
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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 .
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1 Cited Publications
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BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
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γ-Glu-Tyr is an orally active gut microbiota-derived metabolite and a competitive DPP-IV inhibitor with an IC50 of 6.77 mM against hDPP-IV. γ-Glu-Tyr weakly activates hCaSR. γ-Glu-Tyr decreases colonic pro-inflammatory cytokine (IL-6, IL-1β, TNF-α) levels. γ-Glu-Tyr activates the cAMP/PKA signaling pathway and inhibits NF-κB phosphorylation, thereby reducing inflammatory responses. γ-Glu-Tyr can be used for research on type 2 diabetes and ulcerative colitis .
Cat. No.: HY-159829
CAS No.: 1803346-98-6
Synonyms: NBI-1117568; HTL-0016878
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
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 .
CCX-777 is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 is widely used in cancer-related research .
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 .
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HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
Cat. No.: HY-178234
CAS No.: 1892576-07-6
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LY237 is a potent GPR84 full agonist, with EC50 values of 0.189 nM and 0.07 nM in cAMP inhibition assay and calcium flux assay, respectively. LY237 binds to the amphipathic orthosteric pocket of GPR84, stabilizes the active conformation of the receptor, and promotes its coupling with Gαi protein. LY237 can be used in research related to ulcerative colitis, fibrotic diseases, non-alcoholic steatohepatitis, and acute respiratory distress syndrome .
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MOMBA is a selective FFA2 (Free Fatty Acid Receptor 2) orthosteric agonist that activates receptor signaling pathways by binding to the orthosteric site of FFA2 with high specificity. MOMBA holds potential for research on metabolic and inflammatory diseases .
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LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
Cat. No.: HY-103549
CAS No.: 103439-17-4
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Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .
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(R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .
Cat. No.: HY-175168
CAS No.: 2138299-43-9
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diABZI-a1 is a orthosteric STING agonist with EC50 of 117 nM for IFNβ in human PBMCs. diABZI-a1 can be used for monogenic autoinflammatory disease like SAVI disease research .
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LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury .
Cat. No.: HY-175166
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BMS-025 is a orthosteric STING agonist. BMS-025 can induces chemical shift of STING M271 residue, further activating STING IFN signaling. BMS-025 can be used for monogenic autoinflammatory disease like SAVI disease research .
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-13239A
CAS No.: 1311385-35-9
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LY2979165 free base is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
Cat. No.: HY-103551A
CAS No.: 852679-76-6
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LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively .
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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
