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receptor selectivity

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-117139

    Cannabinoid Receptor Neurological Disease
    NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor .
    NESS 0327
  • HY-101348
    L-741626
    1 Publications Verification

    Dopamine Receptor Neurological Disease
    L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
    L-741626
  • HY-107606A

    iGluR Neurological Disease
    UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ~30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine .
    UBP301 hydrochloride
  • HY-135542
    NBI-27914
    2 Publications Verification

    CRFR Others
    NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily .
    NBI-27914
  • HY-115413

    mAChR Neurological Disease
    LG50643 is a potent and selective M3 muscarinic receptor antagonist (pKi=8.64).
    LG50643
  • HY-115953

    Dopamine Receptor Neurological Disease
    Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM) .
    Dopamine D3 receptor ligand-1
  • HY-124117

    5-HT Receptor Neurological Disease
    LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors .
    LY 278584
  • HY-107606

    iGluR Neurological Disease
    UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine .
    UBP301
  • HY-151230

    Estrogen Receptor/ERR Cancer
    (-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer .
    (-)-Erteberel
  • HY-101348R

    Reference Standards Dopamine Receptor Neurological Disease
    L-741626 (Standard) is the analytical standard of L-741626. This product is intended for research and analytical applications. L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
    L-741626 (Standard)
  • HY-135542R

    CRFR Others
    NBI-27914 (Standard) is the analytical standard of NBI-27914. This product is intended for research and analytical applications. NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily .
    NBI-27914 (Standard)
  • HY-P5158

    Adrenergic Receptor Others
    Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
    Conopeptide rho-TIA
  • HY-151413
    MEN 10207
    1 Publications Verification

    Neurokinin Receptor Neurological Disease
    MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
    MEN 10207
  • HY-101327

    Corwin; ICI 118587

    Adrenergic Receptor Cardiovascular Disease
    Xamoterol is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol has the potential for the research of arrhythmogenesis. Xamoterol has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
    Xamoterol
  • HY-103162

    Adenosine Receptor Neurological Disease
    ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease .
    ANR94
  • HY-101327A

    Corwin hemifumarate; ICI 118587 hemifumarate

    Adrenergic Receptor Cardiovascular Disease
    Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
    Xamoterol hemifumarate
  • HY-132811

    CORT113176

    Glucocorticoid Receptor Neurological Disease Inflammation/Immunology
    Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders .
    Dazucorilant
  • HY-12245
    SB-366791
    5+ Cited Publications

    TRP Channel Inflammation/Immunology
    SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation .
    SB-366791
  • HY-108495
    CYM50308
    1 Publications Verification

    ML248

    LPL Receptor Cardiovascular Disease
    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .
    CYM50308
  • HY-101250

    MDL11939

    Serotonin Transporter Neurological Disease
    Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
    Glemanserin
  • HY-175442

    iGluR Neurological Disease
    GluN1/3A-IN-2 (Compound DD-1) is a selective GluN1/GluN3A NMDA receptor inhibitor with an IC50 of 1.26  μM for GluN1/GluN3A NMDA receptor. GluN1/3A-IN-2 can be used for neurological and psychiatric disorders research .
    GluN1/3A-IN-2
  • HY-117378

    KRP-204

    Adrenergic Receptor Inflammation/Immunology Cancer
    N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus .
    N-5984
  • HY-103510

    GABA Receptor Neurological Disease
    TB-21007 is a selective and brain penetrant α5 subunit-containing GABAA receptor inverse agonist with Kis of 1.6 nM, 20 nM, 16 nM, and 20 nM for α5, α1, α2 and α3 subtypes, respectively. TB-21007 enhances cognition in rats .
    TB-21007
  • HY-101250R

    MDL11939 (Standard)

    Reference Standards Serotonin Transporter Neurological Disease
    Glemanserin (Standard) is the analytical standard of Glemanserin. This product is intended for research and analytical applications. Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
    Glemanserin (Standard)
  • HY-118301

    GABA Receptor Neurological Disease
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
    ADX71441
  • HY-173251S

    GABA Receptor Neurological Disease
    ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .
    ENX-101
  • HY-107669

    nAChR Neurological Disease
    nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1 hydrochloride
  • HY-177278

    Somatostatin Receptor Neurological Disease Endocrinology Cancer
    SST1 receptor antagonist-1 (Compound 23) is a selective Somatostatin receptor 1 (SST1) antagonist with pKds of 9.11 and 8.79 for rSST1 and hSST1, respectively. SST1 receptor antagonist-1 can be used for retinal and endocrine dysfunctions, cancer and neuropsychiatric disorders research .
    SST1 receptor antagonist-1
  • HY-171048

    Androgen Receptor Endocrinology Cancer
    GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI) .
    GTx-027
  • HY-19927A

    5-HT Receptor Neurological Disease Endocrinology
    DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
    DA-6886 monohydrochloride
  • HY-151129

    nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1
  • HY-118944

    Adrenergic Receptor Endocrinology
    L-748328 is a potent and selective human β3-adrenergic receptor antagonist. L-748328 has a Ki of 3.7 nM against human cloned β3-AR expressed in Chinese hamster ovary (CHO) cells. In addition, L-748328 inhibits the lipolytic response induced by the β3-AR agonist L-742791 in isolated non-human primate adipocytes .
    L-748328
  • HY-145341

    Estrogen Receptor/ERR Cancer
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
    GNE-149
  • HY-A0037
    Lasofoxifene
    4 Publications Verification

    CP-336156

    Estrogen Receptor/ERR Inflammation/Immunology Cancer
    Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
    Lasofoxifene
  • HY-114732

    Adrenergic Receptor Others
    Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes .
    Procaterol
  • HY-101119

    Estrogen Receptor/ERR Cancer
    GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
    GLL398
  • HY-158102

    ORIC-944

    Histone Methyltransferase Cancer
    Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
    Rinzimetostat
  • HY-A0038
    Lasofoxifene tartrate
    4 Publications Verification

    CP-336156 tartrate

    Estrogen Receptor/ERR Endocrinology Cancer
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
    Lasofoxifene tartrate
  • HY-A0037R

    Estrogen Receptor/ERR Inflammation/Immunology Cancer
    Lasofoxifene (Standard) is the analytical standard of Lasofoxifene. This product is intended for research and analytical applications. Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
    Lasofoxifene (Standard)
  • HY-A0036
    Bazedoxifene acetate
    10+ Cited Publications

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
    Bazedoxifene acetate
  • HY-A0031
    Bazedoxifene
    10+ Cited Publications

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
    Bazedoxifene
  • HY-100554
    BMY 7378
    2 Publications Verification

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
    BMY 7378
  • HY-A0031A

    TSE-424 hydrochloride

    Estrogen Receptor/ERR Cancer
    Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .
    Bazedoxifene hydrochloride
  • HY-158102A

    ORIC-944 TFA

    Histone Methyltransferase Cancer
    Rinzimetostat (ORIC-944) TFA is the TFA salt form of ORIC (HY-158102). Rinzimetostat TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .
    Rinzimetostat TFA
  • HY-A0036R

    TSE-424 acetate (Standard)

    Reference Standards Estrogen Receptor/ERR Cancer
    Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
    Bazedoxifene acetate (Standard)
  • HY-A0031R

    TSE-424 (Standard)

    Reference Standards Estrogen Receptor/ERR Cancer
    Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
    Bazedoxifene (Standard)
  • HY-46531

    Ligands for E3 Ligase Inflammation/Immunology Cancer
    Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1) .
    Thalidomide-5-NH2-CH2-COOH
  • HY-178945

    Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor Neurological Disease Inflammation/Immunology
    KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .
    KOR agonist 7
  • HY-161398

    TGF-β Receptor TGF-beta/Smad Cancer
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research .
    TGFβRII-IN-3
  • HY-178760

    5-HT Receptor Neurological Disease
    TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression) .
    TGF-8027

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