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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
99 Results for "
Orthosteric
" in MedChemExpress (MCE) Product Catalog:
Products (99)
99 Results for "Orthosteric" in MCE Product Catalog:
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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(-)-(S)-B-973B is an allosteric activator of α7 nicotinic acetylcholine receptor (α7 nAChR). (-)-(S)-B-973B alleviates pain behaviors. (-)-(S)-B-973B can be used for the research of inflammatory pain .
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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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-174802
CAS No.: 3117797-77-7
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XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
Cat. No.: HY-N7683
CAS No.: 89595-66-4
Category:
Flavonoids Monophenols Rosaceae Metabolic Disease Phenols Plants Prunus avium Disease Research Fields Isoflavones
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Cat. No.: HY-170805
CAS No.: 1327276-39-0
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UNC0737 is an orthosteric choline kinase inhibitor. UNC0737 is also a poor inhibitor of G9a (IC50 = 5000 nM) and GLP (IC50 > 10000 nM) in the SAHH-coupled assays .
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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-112874
CAS No.: 847998-92-9
Synonyms: BMS-687681
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BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .
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KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively .
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 .
Cat. No.: HY-176783
CAS No.: 3080315-83-6
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GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research .
Cat. No.: HY-124956
CAS No.: 957136-80-0
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GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research .
Cat. No.: HY-146201
CAS No.: 2511632-25-8
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PDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression .
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 .
Cat. No.: HY-120694
CAS No.: 1355454-05-5
Synonyms: RUC-2
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ML165 (RUC-2) is an aIIbb3 receptor antagonist. ML165 has orthosteric inhibition effect at the RGD binding domain. ML165 inhibits platelet adhesion to fibrinogen, and inhibits platelet aggregation (IC50: 96 nM) .
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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 .
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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 .
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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
