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antagonistic activity

" in MedChemExpress (MCE) Product Catalog:

910

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2

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1

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66

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4

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2276A
    Pep2-8 TFA

    		PCSK9 Cardiovascular Disease Others
    Pep2-8 is a peptide which has enhanced the antagonistic activity of proprotein convertase subtilin/ kexin 9 type (PCSK9) .
    Pep2-8 TFA
  • HY-12129
    CP 154526 hydrochloride

    		CFTR Neurological Disease
    CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 hydrochloride has anxiolytic activities .
    CP 154526 hydrochloride
  • HY-100797
    (RS)-CPP

    (±)-CPP

    		 iGluR Neurological Disease
    (RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity .
    (RS)-CPP
  • HY-120997
    E6 Berbamine

    Berbamine p-nitrobenzoate

    		 Calmodulin Cancer
    E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activity of calmodulin (CaM)-dependent myosin light chain kinase (MLCK), with a Ki of 0.95 μM . E6 Berbamine also shows anti-leukemia activities, with an IC50 of 2.13 μM in K562 cells .
    E6 Berbamine
  • HY-12130
    CP 154526

    		CRFR Neurological Disease
    CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities .
    CP 154526
  • HY-108480
    SDZ NKT 343

    		Neurokinin Receptor Neurological Disease
    SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity .
    SDZ NKT 343
  • HY-106499A
    Sulfinalol hydrochloride

    		Adrenergic Receptor Cardiovascular Disease
    Sulfinalol hydrochloride is an orally active β-adrenoceptor antagonist with direct vasodilator activity. Sulfinalol hydrochloride is an antihypertensive agent .
    Sulfinalol hydrochloride
  • HY-107626
    ATC0065

    		MCHR1 (GPR24) 5-HT Receptor Neurological Disease
    ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities .
    ATC0065
  • HY-112741
    SB-209247

    		Leukotriene Receptor Inflammation/Immunology
    SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca 2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity .
    SB-209247
  • HY-107626A
    ATC0065 free base

    		MCHR1 (GPR24) 5-HT Receptor Neurological Disease
    ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities .
    ATC0065 free base
  • HY-P10550
    VGB4

    		VEGFR Cancer
    VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research .
    VGB4
  • HY-106684
    Ridazolol

    		Adrenergic Receptor Cardiovascular Disease
    Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
    Ridazolol
  • HY-106684A
    Ridazolol hydrochloride

    		Adrenergic Receptor Cardiovascular Disease
    Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
    Ridazolol hydrochloride
  • HY-14863
    Lunacalcipol

    CTA-018

    		 VD/VDR Cytochrome P450 Others Endocrinology
    Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
    Lunacalcipol
  • HY-120767
    Linzagolix choline

    KLH-2109 choline; OBE-2109 choline

    		 GnRH Receptor Inflammation/Immunology Cancer
    Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
    Linzagolix choline
  • HY-19037
    SM-2470

    		Adrenergic Receptor Cardiovascular Disease Neurological Disease Metabolic Disease
    SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats . SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization .
    SM-2470
  • HY-147560
    σ1 Receptor/μ Opioid receptor modulator 1

    		Sigma Receptor Opioid Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .
    σ1 Receptor/μ Opioid receptor modulator 1
  • HY-145258
    GABAA receptor agent 6

    		GABA Receptor Neurological Disease
    GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
    GABAA receptor agent 6
  • HY-148494
    Tivumecirnon

    FLX475

    		 CCR Inflammation/Immunology Cancer
    Tivumecirnon (FLX475) is an orally bioactive, selective CCR4 antagonist. Tivumecirnon can block the recruitment of immunosuppressive regulatory T cells (Treg) into the tumor microenvironment, leading to enhanced antitumor activity. Tivumecirnon has antitumor activity on EBV+ NK/T cell lymphoma and non-small cell lung cancer (NSCLC) combined with Pembrolizumab (HY-P9902). Tivumecirnon is promising for research of broad range of tumor types .
    Tivumecirnon
  • HY-106056
    Zindoxifene

    D 16726

    		 Others Cancer
    Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
    Zindoxifene
  • HY-107551
    GLI antagonist-1

    		Gli Cancer
    GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
    GLI antagonist-1
  • HY-126806
    Pyrrofolic acid

    		Antibiotic Cancer
    Pyrrofolic acid is a folate antagonist with a low activity as a folate antagonist for Streptococcus faecalis .
    Pyrrofolic acid
  • HY-136437
    CXCR4 antagonist 1

    		CXCR HIV Infection
    CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity .
    CXCR4 antagonist 1
  • HY-143253
    Estrogen receptor antagonist 7

    		Estrogen Receptor/ERR Cancer
    Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
    Estrogen receptor antagonist 7
  • HY-119832B
    (S)-Setastine

    (S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid

    		 Histamine Receptor Inflammation/Immunology
    (S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases .
    (S)-Setastine
  • HY-148259
    SF-1 antagonist-1

    		Orphan Receptor Cancer
    SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer .
    SF-1 antagonist-1
  • HY-149967
    GluN2B-NMDAR antagonist-1

    		iGluR Neurological Disease Inflammation/Immunology
    GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury .
    GluN2B-NMDAR antagonist-1
  • HY-146027
    Androgen receptor antagonist 4

    		Androgen Receptor Cancer
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .
    Androgen receptor antagonist 4
  • HY-146026
    Androgen receptor antagonist 3

    		Androgen Receptor Cancer
    Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities .
    Androgen receptor antagonist 3
  • HY-157939
    GPR183 antagonist-3

    		EBI2/GPR183 Inflammation/Immunology
    GPR183 antagonist-3 (compound 33) is an oral active GPR183 antagonist with the IC50 of 8.7 μM. GPR183 antagonist-3 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, and improves the pathological symptoms of DSS-induced experimental colitis .
    GPR183 antagonist-3
  • HY-169941
    ERα/ERβ antagonist-1

    		Estrogen Receptor/ERR Metabolic Disease Cancer
    ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells .
    ERα/ERβ antagonist-1
  • HY-131868
    TRPV3 antagonist 74a

    		TRP Channel Neurological Disease
    TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain .
    TRPV3 antagonist 74a
  • HY-144377
    RXR antagonist 1

    		RAR/RXR Neurological Disease Metabolic Disease Cancer
    RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research .
    RXR antagonist 1
  • HY-136645
    EP4 receptor antagonist 2

    		Prostaglandin Receptor Cancer
    EP4 receptor antagonist 2 (compound 2-13) is a potent EP4 receptor antagonist with an IC50 of 7.8 nM. EP4 receptor antagonist 2 shows antitumor activity .
    EP4 receptor antagonist 2
  • HY-152131
    CCR5 antagonist 2

    		CCR HIV Infection
    CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities .
    CCR5 antagonist 2
  • HY-152132
    CCR5 antagonist 3

    		CCR HIV Infection
    CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities .
    CCR5 antagonist 3
  • HY-149084
    LTB4 antagonist 3

    		Leukotriene Receptor Inflammation/Immunology
    LTB4 antagonist 3 (compound 24e) is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM. LTB4 antagonist 3 has anti-inflammatory activity .
    LTB4 antagonist 3
  • HY-P10388
    TAX2 peptide

    		CD47 TGF-β Receptor Cancer
    TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
    TAX2 peptide
  • HY-136702
    L-97-1

    		Adenosine Receptor Inflammation/Immunology
    L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
    L-97-1
  • HY-12079
    CP-481715

    		CCR Inflammation/Immunology
    CP-481715 is a potent, reversible and selective CCR1 antagonist with a Kd of 9.2 nM for human CCR1. CP-481715 is >100-fold selective for CCR1 as compared with a panel of G-protein-coupled receptors including related chemokine receptors. CP-481715 has the potential for rheumatoid arthritis and other inflammatory diseases research .
    CP-481715
  • HY-146494
    Androgen receptor antagonist 5

    		Androgen Receptor Cancer
    Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
    Androgen receptor antagonist 5
  • HY-165155
    CysLT1 receptor antagonist-1

    		Leukotriene Receptor Inflammation/Immunology
    CysLT1 receptor antagonist-1 (Compound 4) is an antagonist for cysteinyl leukotriene receptor 1 (CysLT1R) with an IC50 of 3.9 μM. CysLT1 receptor antagonist-1 exhibits weak agonist activity against G-protein-coupled bile acid receptor 1 (GPBAR1) with an efficact of 23% at 10 μM. CysLT1 receptor antagonist-1 can be used for asthma and allergic diseases researchs .
    CysLT1 receptor antagonist-1
  • HY-118914
    Glucagon receptor antagonist inactive control

    		GCGR
    Glucagon receptor antagonist inactive control (Compound 2) is a compound structurally similar to the glucagon receptor (GCGR) antagonist Glucagon receptor antagonist (Compound 1) but lacks antagonistic activity against glucagon receptor (GCGR). Glucagon receptor antagonist inactive control can be used as a negative control to study mechanisms related to glucagon receptor-mediated signaling pathways .
    Glucagon receptor antagonist inactive control
  • HY-101691
    Ecastolol

    		Adrenergic Receptor Cardiovascular Disease Endocrinology
    Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
    Ecastolol
  • HY-137175
    TMBIM6 antagonist-1

    		mTOR Cancer
    TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+ .
    TMBIM6 antagonist-1
  • HY-149083
    LTB4 antagonist 2

    		Leukotriene Receptor Inflammation/Immunology
    LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. LTB4 antagonist 2 shows good affinity for the LTB4 receptor with IC50 of 439 nM .
    LTB4 antagonist 2
  • HY-163504
    PAR4 antagonist 5

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    PAR4 antagonist 5 (compound 1) is a PAR4 antagonist with an IC50 less than 20 μM and potent anti-platelet aggregation activity. PAR4 antagonist 5 can be used for research of thrombosis disease .
    PAR4 antagonist 5
  • HY-101743
    Elucaine

    		mAChR Inflammation/Immunology
    Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
    Elucaine
  • HY-U00350
    CCX354
    1 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology
    CCX354 is an antagonist of CCR1, with anti-inflammatory activity.
    CCX354
  • HY-160680
    AR antagonist 6

    		Androgen Receptor Endocrinology
    AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model .
    AR antagonist 6

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