2. Search Result
Search Result
Results for "

agonism

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148212
    GLP-1R agonist 17

    		GCGR Cardiovascular Disease Metabolic Disease
    GLP-1R agonist 17 is a GLP-1 receptor agonist. GLP-1R agonist 17 shows excellent agonism on a GLP-1 receptor. GLP-1R agonist 17 can be used for the research of cardiovascular metabolic diseases .
    GLP-1R agonist 17
  • HY-119486A
    (Rac)-Tavapadon

    (Rac)-PF-06649751; (Rac)-CVL-751

    		 Dopamine Receptor Arrestin Neurological Disease
    (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
    (Rac)-Tavapadon
  • HY-164128
    AHL modulator-1

    		Others Others
    AHL modulator-1 (compound 12) is a modulator of N-acylated L-homoserine lactone (AHL), with the agonism and antagonism of 21% and 42% in cellulase activity and 5% and 32% in potato macerationa, respectively .
    AHL modulator-1
  • HY-146731
    PPARγ agonist 1

    		PPAR Cardiovascular Disease Metabolic Disease
    PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders .
    PPARγ agonist 1
  • HY-139678
    SC13

    		Opioid Receptor Others
    SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.
    SC13
  • HY-146288
    LXR agonist 2

    		LXR Metabolic Disease
    LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism .
    LXR agonist 2
  • HY-125839
    OP-3633

    		Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
    OP-3633
  • HY-151515
    Dopamine D2 receptor agonist-2

    		Dopamine Receptor Neurological Disease
    Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D2 receptor biased agonism ligand with an Ki value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis .
    Dopamine D2 receptor agonist-2
  • HY-P4764
    Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2

    		Melanocortin Receptor Cardiovascular Disease
    Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 is a cyclic octapeptide with MC4R agonism. Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 significantly increases heart rate and blood pressure .
    Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
  • HY-155706
    MOR agonist-2

    		Opioid Receptor Dopamine Receptor Inflammation/Immunology
    MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
    MOR agonist-2
  • HY-U00443
    SB 258719

    		5-HT Receptor Neurological Disease Cancer
    SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
    SB 258719
  • HY-103123
    SB 258719 hydrochloride

    		5-HT Receptor Neurological Disease Cancer
    SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases .
    SB 258719 hydrochloride
  • HY-123123
    RS-61756-007

    		Others Cardiovascular Disease
    RS-61756-007 is a selective thromboxane receptor (TP) agonist with high activity at the TP receptor. RS-61756-007 showed agonism at TP and FP receptors in in vitro studies but had no activity at other receptor subtypes. The effects of RS-61756-007 can be antagonized in a similar manner by the TP antagonist SQ 29,548 .
    RS-61756-007
  • HY-145153
    S-777469

    		Cannabinoid Receptor Neurological Disease
    S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
    S-777469
  • HY-147705
    PPARγ phosphorylation inhibitor 1

    		PPAR Metabolic Disease
    PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects .
    PPARγ phosphorylation inhibitor 1
  • HY-149387
    D3R/MOR antagonist 2

    		Dopamine Receptor Opioid Receptor Inflammation/Immunology
    D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
    D3R/MOR antagonist 2
  • HY-149386
    D3R/MOR antagonist 1

    		Dopamine Receptor Opioid Receptor Inflammation/Immunology
    D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
    D3R/MOR antagonist 1
  • HY-141852
    STAMBP-IN-1

    		Deubiquitinase Inflammation/Immunology
    STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM .
    STAMBP-IN-1
  • HY-105689
    AGN 192870

    		RAR/RXR Others
    AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism . AGN 192870 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AGN 192870
  • HY-163065
    σ1 Receptor/μ Opioid receptor modulator 2

    		Opioid Receptor Sigma Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-118775
    LEK 8804

    		Others Others
    LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
    LEK 8804
  • HY-114978
    VU0424465

    		mGluR PERK Neurological Disease
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
    VU0424465
  • HY-162585
    5-HT1AR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
    5-HT1AR agonist 1
  • HY-137055
    PF-3774076

    		Others Others
    PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
    PF-3774076

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: