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Orthosteric

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42

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W011417
    Cinnabarinic acid

    		Endogenous Metabolite mGluR Apoptosis Others
    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 .
    Cinnabarinic acid
  • HY-59384
    MOMBA

    		Free Fatty Acid Receptor Metabolic Disease Inflammation/Immunology
    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 .
    MOMBA
  • HY-145300
    nAChR modulator-2

    		nAChR Infection
    nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator .
    nAChR modulator-2
  • HY-145299
    nAChR modulator-1

    		nAChR Infection
    nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator .
    nAChR modulator-1
  • HY-103549
    Z-Cyclopentyl-AP4

    		mGluR Neurological Disease
    Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .
    Z-Cyclopentyl-AP4
  • HY-170805
    UNC0737

    		Choline Kinase Cancer
    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 .
    UNC0737
  • HY-116569
    VU0455691

    		mAChR Cardiovascular Disease
    VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1) .
    VU0455691
  • HY-147559
    CB1R Allosteric modulator 2

    		Cannabinoid Receptor Others
    CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
    CB1R Allosteric modulator 2
  • HY-147558
    CB1R Allosteric modulator 1

    		Cannabinoid Receptor Others
    CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
    CB1R Allosteric modulator 1
  • HY-103513
    GABAA receptor agent 2

    		GABA Receptor Others
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-176550
    ASIC1a antagonist-1

    		Sodium Channel Neurological Disease
    ASIC1a antagonist-1 (Compound 5b) is an orthosteric noncompetitive Acid sensing ion channels 1a (ASIC1a) antagonist with an IC50 of 27 nM (pH 6.7). ASIC1a antagonist-1 shifts pH dependence of ASIC1a activation and inhibits its maximal evoked response. ASIC1a antagonist-1 completely inhibits long-term potentiation (LTP) induction in CA3-CA1 pathway. ASIC1a antagonist-1 can be used for brain diseases and pathologies research .
    ASIC1a antagonist-1
  • HY-112247
    SR 16832

    		PPAR Metabolic Disease
    SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .
    SR 16832
  • HY-13239
    LY2979165

    		mGluR Neurological Disease
    LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
    LY2979165
  • HY-112874
    BMS-681

    		CCR Neurological Disease Inflammation/Immunology Cancer
    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 .
    BMS-681
  • HY-13239A
    LY2979165 free base

    		mGluR Neurological Disease
    LY2979165 free base is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist .
    LY2979165 free base
  • HY-138694
    5-Benzyloxygramine

    		Antibiotic Infection
    5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities .
    5-Benzyloxygramine
  • HY-P10051
    Cyclorasin 9A5

    		Ras Raf Cancer
    Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM .
    Cyclorasin 9A5
  • HY-P10051A
    Cyclorasin 9A5 TFA

    		Ras Raf Cancer
    Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM .
    Cyclorasin 9A5 TFA
  • HY-176487
    SARM1-IN-6

    		Toll-like Receptor (TLR) Neurological Disease
    SARM1-IN-6 (Compound 17a) is a brain-permeable SARM1 orthosteric inhibitor with IC50 of 14 nM for NAM and 74 nM for HEK cells .
    SARM1-IN-6
  • HY-162659
    β2AR ligand 1

    		Adrenergic Receptor Others
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS) .
    β2AR ligand 1
  • HY-119943B
    (R)-PF-06256142

    		Dopamine Receptor Neurological Disease
    (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 .
    (R)-PF-06256142
  • HY-10915
    LUF6096

    		Adenosine Receptor Cardiovascular Disease
    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 .
    LUF6096
  • HY-103551A
    LY 541850

    		mGluR Neurological Disease
    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 .
    LY 541850
  • HY-142972
    19(S)-HETE

    		Prostaglandin Receptor Cardiovascular Disease
    19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .
    19(S)-HETE
  • HY-150147
    CAM833
    1 Publications Verification

    		 RAD51 Apoptosis Cancer
    CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a Kd of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .
    CAM833
  • HY-122491
    Dimethyl-W84 dibromide

    		mAChR Neurological Disease
    Dimethyl-W84 (dibromide) modulates M2 muscarinic acetylcholine receptors. Dimethyl-W84 (dibromide) can be used in nervous system related research .
    Dimethyl-W84 dibromide
  • HY-W011417R
    Cinnabarinic acid (Standard)

    		Endogenous Metabolite Reference Standards mGluR Apoptosis Others
    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 .
    Cinnabarinic acid (Standard)
  • HY-12150
    CCMI
    1 Publications Verification

    AVL-3288; UCI-4083

    		 nAChR Neurological Disease
    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 .
    CCMI
  • HY-174147
    GABAB receptor antagonist 4

    		GABA Receptor Neurological Disease
    GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .
    GABAB receptor antagonist 4
  • HY-117444
    ONO-9780307

    		LPL Receptor Cancer
    ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC50 value of 2.7 nM .
    ONO-9780307
  • HY-117764
    LSP4-2022

    		mGluR Neurological Disease
    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 .
    LSP4-2022
  • HY-174801
    XL-3156

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    XL-3156 is a potent, selective, and cross-species cGAS inhibitor. XL-3156 can simultaneously occupy both allosteric and orthosteric sites, and inhibit the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of autoimmune diseases, inflammatory conditions and other diseases .
    XL-3156
  • HY-172660
    36R-D481

    		Interleukin Related Inflammation/Immunology
    36R-D481 is a competitive and orthosteric antagonist of IL-36R, effectively inhibiting IL-36 signaling. 36R-D481 can inhibit IL-36α and IL-36γ but not IL-36β induced IL-8 release .
    36R-D481
  • HY-120645
    BMS-986122
    1 Publications Verification

    		 Opioid Receptor Neurological Disease
    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 .
    BMS-986122
  • HY-124634
    PZ-2891
    1 Publications Verification

    		 Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
    PZ-2891
  • HY-131032
    KI-7

    		Adenosine Receptor Others
    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 .
    KI-7
  • HY-144705
    GAT564

    		Cannabinoid Receptor Neurological Disease
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
    GAT564
  • HY-148502
    VU6019650
    2 Publications Verification

    		 mAChR Neurological Disease
    VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
    VU6019650
  • HY-158104
    LPPM-8

    		ATF6 Others
    LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .
    LPPM-8
  • HY-156025
    HCAR2 agonist 1

    		Hydroxycarboxylic Acid Receptor (HCAR) Inflammation/Immunology
    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 .
    HCAR2 agonist 1
  • HY-126242S
    Tyk2-IN-7

    		JAK Inflammation/Immunology
    Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model .
    Tyk2-IN-7
  • HY-174802
    XL-3158

    		Cyclic GMP-AMP Synthase IKK IFNAR Inflammation/Immunology
    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 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases.
    XL-3158

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