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Receptor modulator

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-A0036
    Bazedoxifene acetate
    15+ 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
    15+ Cited Publications

    TSE-424

    Estrogen Receptor/ERR Neurological Disease 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-A0037
    Lasofoxifene
    5 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-116330A
    Hyperforin dicyclohexylammonium salt
    3 Publications Verification

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease Cancer
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
    Hyperforin dicyclohexylammonium salt
  • HY-10933
    CX516
    2 Publications Verification

    BDP 12

    iGluR Neurological Disease
    CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .
    CX516
  • HY-16716
    Basmisanil
    1 Publications Verification

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
    Basmisanil
  • HY-122025
    AC-262536
    1 Publications Verification

    Androgen Receptor Metabolic Disease
    AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
    AC-262536
  • HY-101165
    Cyclothiazide
    2 Publications Verification

    iGluR GABA Receptor Neurological Disease
    Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
    Cyclothiazide
  • HY-15618

    M1 Receptor modulator

    mAChR Calcium Channel Neurological Disease
    MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
    MK-7622
  • HY-139580

    CAD-9303

    iGluR Neurological Disease
    Plazinemdor (CAD-9303) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptors, which is used in the research of neurological diseases .
    Plazinemdor
  • HY-A0038
    Lasofoxifene tartrate
    5 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-179738

    CGRP Receptor Amylin Receptor Metabolic Disease
    CTR/AMYR modulator-1 is a calcitonin receptor/amylin receptor modulator. CTR/AMYR modulator-1 can be used for the research of metabolic disease .
    CTR/AMYR modulator-1
  • HY-139897

    iGluR Neurological Disease
    CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD) .
    CX 717
  • HY-116553

    Wnt β-catenin Cancer
    FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .
    FzM1
  • HY-177873

    iGluR Neurological Disease
    AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC50 = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia .
    AMPA receptor modulator-10
  • HY-110201

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
    Estrogen receptor modulator 1
  • HY-10018

    Toll-like Receptor (TLR) Inflammation/Immunology
    Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
    Toll-like receptor modulator
  • HY-151876

    Glucocorticoid Receptor NF-κB AP-1 Inflammation/Immunology
    Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice .
    Glucocorticoid receptor modulator 1
  • HY-136275

    iGluR Others
    AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ8 dependent AMPA receptor . pIC50 = -lgIC50.
    AMPA receptor modulator-2
  • HY-153584

    GABA Receptor Neurological Disease
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
    MRK-898
  • HY-130630

    mGluR Neurological Disease
    mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
    mGluR2 modulator 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-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-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-144291

    Dopamine Receptor Neurological Disease
    LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
    LY3154885
  • HY-117851

    CaSR Metabolic Disease Endocrinology
    AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .
    AC-265347
  • HY-112567

    Adenosine Receptor Neurological Disease
    TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management .
    TRR469
  • HY-177275

    c-Kit Cancer
    c-Kit Receptor modulator-1 (Compound #22) is a c-Kit Receptor modulator. c-Kit Receptor modulator-1 can be used for malignant cancers such as canine mastocytoma, human gastrointestinal stromal tumor and small cell lung cancer research .
    c-Kit Receptor modulator-1
  • HY-155628

    iGluR Others
    AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .
    AMPA receptor modulator-6
  • HY-163673

    Glucocorticoid Receptor Drug-Linker Conjugates for ADC Inflammation/Immunology
    Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models .
    Glucocorticoid receptor modulator 4
  • HY-153458

    Orexin Receptor (OX Receptor) Cardiovascular Disease Neurological Disease Metabolic Disease
    Orexin receptor modulator-1 is an orexin receptor modulator. Orexin receptor modulator-1 can be used for the research of substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension .
    Orexin receptor modulator-1
  • HY-U00429

    Nuclear Hormone Receptor 4A/NR4A Neurological Disease
    NOT Receptor Modulator 1 is a nuclear receptor Nurr-1/NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
    NOT Receptor Modulator 1
  • HY-161090

    iGluR Neurological Disease
    AMPA receptor modulator-7 (compound 36) is a modulator of AMPA receptor. AMPA receptor modulator-7 has oral activity and can penetrate the blood-brain barrier .
    AMPA receptor modulator-7
  • HY-113689

    Cannabinoid Receptor Neurological Disease
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
    GAT211
  • HY-N12744

    Glucocorticoid Receptor Metabolic Disease
    2-O-trans-p-Coumaroylalphitolic acid (Zj7) is a triterpene which can be extracted from jujube plants. 2-O-trans-P-Coumaroyl alphitolic acid is a selective modulator of glucocorticoid receptor (GR). 2-O-trans-P-coumaroyl alphitolic acid can be used in the study of obesity .
    2-O-trans-p-Coumaroylalphitolic acid
  • HY-109572

    GABA Receptor Neurological Disease
    GABAA receptor modulator-1 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases .
    GABAA receptor modulator-1
  • HY-175508

    iGluR Neurological Disease
    NMDA receptor modulator 9 is an orally active NMDA receptor positive allosteric modulator (PAM). NMDA receptor modulator 9 enhances GluN2A receptor activity. NMDA receptor modulator 9 demonstrates significant antidepressant-like effects in chronic restraint stress (CRS)-induced depression mice. NMDA receptor modulator 9 can be used for the study of depression .
    NMDA receptor modulator 9
  • HY-143390

    iGluR Neurological Disease
    NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research .
    NMDA receptor modulator 2
  • HY-143396

    iGluR Neurological Disease
    NMDA receptor modulator 5 (Compound 195) is a potent NMDA receptor modulator. NMDA receptor modulator 5 can be used for neurological disorder research .
    NMDA receptor modulator 5
  • HY-143393

    iGluR Neurological Disease
    NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research .
    NMDA receptor modulator 4
  • HY-143391

    iGluR Neurological Disease
    NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator. NMDA receptor modulator 3 can be used for neurological disorder research .
    NMDA receptor modulator 3
  • HY-143397

    iGluR Neurological Disease
    NMDA receptor modulator 6 (Compound 183) is a potent NMDA receptor modulator. NMDA receptor modulator 6 can be used for neurological disorder research .
    NMDA receptor modulator 6
  • HY-149165

    Glucocorticoid Receptor Inflammation/Immunology
    Glucocorticoid receptor modulator 2 (Example 1) is a glucocorticoid receptor modulator, with an IC50 value less than 100 nM. Glucocorticoid receptor modulator 2 can be used for research of inflammatory and immune diseases .
    Glucocorticoid receptor modulator 2
  • HY-154798

    iGluR Neurological Disease
    AMPA receptor modulator-5 (Example 217) is an AMPA receptor modulator. AMPA receptor modulator-5 can be used for research of neurological disease .
    AMPA receptor modulator-5
  • HY-171049

    Androgen Receptor Cardiovascular Disease
    Androgen receptor modulator 3 is a selective modulator for androgen receptor that can be used for research of sarcopenia .
    Androgen receptor modulator 3
  • HY-160931

    iGluR Neurological Disease
    NMDA receptor modulator 8 (Compound 3-6) is a modulator for NMDA receptor, with 50%-100% potentiation of NMDA receptor at 10 μM .
    NMDA receptor modulator 8
  • HY-163672

    Glucocorticoid Receptor Metabolic Disease Inflammation/Immunology
    Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases .
    Glucocorticoid receptor modulator 3
  • HY-122150

    iGluR Neurological Disease
    AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC50: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory .
    AMPA receptor modulator-3
  • HY-170902

    GABA Receptor Neurological Disease
    GABAA receptor modulator-4 (Compound 4) is the negative allosteric modulator for GABAA receptor. GABAA receptor modulator-4 inhibits α1β3γ2 GABAA receptor-mediated peak and steady currents with IC50 of 10 μM and 10 μM .
    GABAA receptor modulator-4
  • HY-U00420

    Opioid Receptor Neurological Disease
    Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
    Opioid receptor modulator 1

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