Search Result
Results for "
κ-opioid
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107748
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5'-GNTI hydrochloride
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Opioid Receptor
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Neurological Disease
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5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor .
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- HY-N0050
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(+)-Allomatrine
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Others
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Neurological Disease
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Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors .
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- HY-163017
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- HY-145128
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- HY-P3609
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JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-W019787
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Opioid Receptor
CXCR
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Neurological Disease
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BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
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- HY-10486
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- HY-101231
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ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
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- HY-101205
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ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion .
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- HY-107384
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EMD-61753
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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- HY-107384A
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EMD-61753 hydrochloride
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Opioid Receptor
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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- HY-100963
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U-54494A is a benzamide derivative related to κ-opioid receptor agonists, U-54494A has an anticonvulsant activity .
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- HY-101223
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DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .
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- HY-P1594
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P1594A
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P3647
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- HY-P3647A
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Opioid Receptor
Adenylate Cyclase
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Neurological Disease
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[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
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- HY-P5907
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Opioid Receptor
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Neurological Disease
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Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
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- HY-136208
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Opioid Receptor
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Neurological Disease
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TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
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- HY-101079
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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 .
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- HY-19231
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Org 41793
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Opioid Receptor
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Neurological Disease
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DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
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- HY-110302
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-N7437
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- HY-P5892
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Opioid Receptor
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Neurological Disease
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β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
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- HY-123689
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ALKS-33; RDC-0313
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Opioid Receptor
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Neurological Disease
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Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-P10006
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-P3376
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- HY-100903
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nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
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Opioid Receptor
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Neurological Disease
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Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
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- HY-156614
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- HY-121800
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- HY-P3445
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- HY-P3445A
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- HY-101582
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- HY-P0088
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
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Others
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
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- HY-101718
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- HY-107749
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- HY-117040
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Norbinaltorphimine; NorBNI
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Opioid Receptor
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Others
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nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo .
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- HY-10487
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- HY-135230
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FP3FBZ
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Opioid Receptor
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Neurological Disease
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LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
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- HY-17609
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CR-845; FE-202845
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Opioid Receptor
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Neurological Disease
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Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-P1299
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Opioid Receptor
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Neurological Disease
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UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
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- HY-P3634
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Opioid Receptor
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Neurological Disease
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[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
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- HY-126910
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Opioid Receptor
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Metabolic Disease
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Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
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- HY-P4679
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E2078
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Opioid Receptor
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Neurological Disease
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(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 .
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- HY-163277
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Opioid Receptor
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Inflammation/Immunology
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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 lowβ-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
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- HY-P1333
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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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 .
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- HY-P1299A
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Opioid Receptor
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Neurological Disease
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UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
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- HY-P1333A
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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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 .
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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- HY-124754
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BTRX-335140; CYM-53093
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
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- HY-119733
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Opioid Receptor
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Neurological Disease
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BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
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- HY-N0164
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Matrine
Maximum Cited Publications
12 Publications Verification
Matridin-15-one; Vegard; α-Matrine
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PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
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Inflammation/Immunology
Cancer
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Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
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- HY-19627
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S-297995
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
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- HY-19627A
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S-297995 tosylate
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Opioid Receptor
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Neurological Disease
Metabolic Disease
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Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1594A
-
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P3609
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JNJ 38488502; FE 200665
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Opioid Receptor
|
Neurological Disease
|
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-W019787
-
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Opioid Receptor
CXCR
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Neurological Disease
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BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
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- HY-P1594
-
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Opioid Receptor
iGluR
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Neurological Disease
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Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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- HY-P3647
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- HY-P3647A
-
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Opioid Receptor
Adenylate Cyclase
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Neurological Disease
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[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
|
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- HY-P5907
-
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Opioid Receptor
|
Neurological Disease
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
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- HY-P5892
-
|
Opioid Receptor
|
Neurological Disease
|
β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
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- HY-P10006
-
|
Opioid Receptor
|
Neurological Disease
|
Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
|
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- HY-P3376
-
-
- HY-P3445
-
-
- HY-P3445A
-
-
- HY-P0088
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
|
Others
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
|
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- HY-17609
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CR-845; FE-202845
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Opioid Receptor
|
Neurological Disease
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-P1299
-
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Opioid Receptor
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Neurological Disease
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
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- HY-P3634
-
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Opioid Receptor
|
Neurological Disease
|
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
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- HY-P4679
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E2078
|
Opioid Receptor
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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 .
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- HY-P1333
-
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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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 .
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- HY-P1299A
-
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Opioid Receptor
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Neurological Disease
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UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
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- HY-P1333A
-
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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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 .
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- HY-P10203
-
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P83387
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KOR; R21; KOR-1; MSL-1; Oprk2; K-OR-1
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WB, IP
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Rat |
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