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KOR+Agonist

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

4

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1333
    Dynorphin A
    1 Publications Verification

    		 Opioid Receptor Apoptosis Caspase Endogenous Metabolite Neurological Disease
    Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
    Dynorphin A
  • HY-15997
    (-)-U-50488 hydrochloride
    1 Publications Verification

    (-)-Trans-(1S,2S)-U-50488 hydrochloride

    		 Opioid Receptor Infection Cancer
    (-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
    (-)-U-50488 hydrochloride
  • HY-15997B
    (±)-U-50488 hydrochloride

    (±)-Trans-(1R,2R)-U-50488 hydrochloride

    		 Opioid Receptor Neurological Disease
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (±)-U-50488 hydrochloride
  • HY-101079
    BRL 52537 hydrochloride

    		Opioid Receptor Neurological Disease
    BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
    BRL 52537 hydrochloride
  • HY-170973
    KOR agonist 4

    		Opioid Receptor
    KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
    KOR agonist 4
  • HY-110302
    6'-GNTI dihydrochloride

    		Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
    6'-GNTI dihydrochloride
  • HY-178945
    KOR agonist 7

    		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-15997C
    (±)-U-50488 hydrate hydrochloride

    (±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride

    		 Opioid Receptor Neurological Disease
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (±)-U-50488 hydrate hydrochloride
  • HY-105235
    Enadoline

    CI-977

    		 Opioid Receptor Neurological Disease
    Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
    Enadoline
  • HY-120949
    (1R,2R)-U-50488 hydrochloride

    		Opioid Receptor Neurological Disease
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (1R,2R)-U-50488 hydrochloride
  • HY-106756
    Spiradoline

    U-62066

    		 Opioid Receptor Neurological Disease
    Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
    Spiradoline
  • HY-175486
    KOR agonist 6

    		Opioid Receptor Neurological Disease
    KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [ 35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .
    KOR agonist 6
  • HY-172407
    KOR agonist 5

    		Opioid Receptor Others
    KOR agonist 5 (Compound 10a) is a KOR/MOR modulator with agonistic activity towards KOR and antagonistic activity towards MOR. KOR agonist 5 can effectively block morphine-induced antinociception and inhibition of intestinal motility. KOR agonist 5 can be used in the research of Substance Use Disorder (SUD) .
    KOR agonist 5
  • HY-159088
    KOR agonist 2

    		Opioid Receptor Neurological Disease
    KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
    KOR agonist 2
  • HY-161539
    KOR agonist 1

    		Opioid Receptor Neurological Disease
    KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
    KOR agonist 1
  • HY-B1485
    Nalmefene hydrochloride

    		Opioid Receptor Neurological Disease
    Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .
    Nalmefene hydrochloride
  • HY-171236
    FEKAP

    		Opioid Receptor
    FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (Ki = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. 11C-FEKAP can be utilized as a radiotracer for imaging KOR .
    FEKAP
  • HY-124959
    Spiradoline mesylate

    U-62066 mesylate

    		 Opioid Receptor Neurological Disease
    Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
    Spiradoline mesylate
  • HY-163277
    PIPE-3297

    		Opioid Receptor Inflammation/Immunology
    PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
    PIPE-3297
  • HY-183773
    KOR agonist-9

    		Opioid Receptor Neurological Disease
    KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus .
    KOR agonist-9
  • HY-181515
    KOR agonist 8

    		Opioid Receptor Neurological Disease
    KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .
    KOR agonist 8
  • HY-122169
    Ketazocine

    Ketocyclazocine

    		 Opioid Receptor Neurological Disease
    Ketazocine (Ketocyclazocine) is a selective κ-opioid receptor (KOR) agonist. Ketazocine is promising for research of analgesics and sedatives .
    Ketazocine
  • HY-105235A
    Enadoline hydrochloride

    CI-977 hydrochloride

    		 Opioid Receptor Neurological Disease
    Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
    Enadoline hydrochloride
  • HY-107744R
    Nalmefene (Standard)

    		Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB Reference Standards Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Nalmefene (Standard) is the analytical standard of Nalmefene. This product is intended for research and analytical applications. Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .
    Nalmefene (Standard)
  • HY-P4679
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)

    E2078

    		 Opioid Receptor Neurological Disease
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
  • HY-130696
    (+)-U-50488

    (+)-Trans-(1R,2R)-U-50488

    		 Opioid Receptor Neurological Disease
    (+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
    (+)-U-50488
  • HY-15997A
    (+)-U-50488 hydrochloride

    (+)-Trans-(1R,2R)-U-50488 hydrochloride

    		 Opioid Receptor Neurological Disease
    (+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
    (+)-U-50488 hydrochloride
  • HY-P1333A
    Dynorphin A TFA

    		Opioid Receptor Apoptosis Caspase Endogenous Metabolite Neurological Disease
    Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
    Dynorphin A TFA
  • HY-161812
    MOR agonist-4

    		Opioid Receptor Others
    MOR agonist-4 (2d) is a G protein signaling-biased Kappa opioid receptor (KOR) agonist with an EC50 value of 11 nM. MOR agonist-4 contains an electron withdrawing CF3 group and a bias factor of 38 based on triazole. MOR agonist-4 is used in the research of pruritis and analgesia .
    MOR agonist-4
  • HY-178720
    SHR0687

    		Opioid Receptor Neurological Disease
    SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist with an EC50 of 0.53 pM. SHR0687 displays high potency and selectivity over MOR and DOR, with negligible blood-brain barrier penetration. SHR0687 activates KOR specifically, leading to potential modulation of neurological pathways without significant central nervous system effects. SHR0687 can be used for the research of pain .
    SHR0687
  • HY-P1625
    Daeatal

    Dynorphin A ethylamide (1-9)

    		 Opioid Receptor Neurological Disease
    Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
    Daeatal

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