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anti-nociceptive pain activity

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

2

Peptides

4

Natural
Products

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0826
    Corynoline
    5+ Cited Publications

    Cholinesterase (ChE) Keap1-Nrf2 Heme Oxygenase (HO) COX NO Synthase p38 MAPK JNK Apoptosis Bcl-2 Family Caspase STAT Interleukin Related Neurological Disease Inflammation/Immunology Cancer
    Corynoline is an orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits multiple activities including anti-inflammatory, antinociceptive, antitumor and analgesic effects. Corynoline can be used in the research of diseases such as tumors and inflammatory pain .
    Corynoline
  • HY-117626
    LP-935509
    1 Publications Verification

    AAK1 Cyclin G-associated Kinase (GAK) SARS-CoV Infection Neurological Disease Inflammation/Immunology
    LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
    LP-935509
  • HY-18099
    S1RA
    3 Publications Verification

    E-52862

    Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
    S1RA
  • HY-131004

    Cannabinoid Receptor Neurological Disease
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
    CB2R PAM
  • HY-101290A

    Cyclin G-associated Kinase (GAK) AAK1 Neurological Disease
    BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
    BMT-090605 hydrochloride
  • HY-N9502

    Endogenous Metabolite Neurological Disease
    Linalool oxide is a monoterpene and found in aromatic plant essential oils and is a secondary metabolite in elongating wheat plants. Linalool oxide has antinociceptive, anticonvulsant, and anxiolytic activity. Linalool oxide can be used for the research of pain, epilepsy, anxiety disorders .
    Linalool oxide
  • HY-151391

    Biochemical Assay Reagents Neurological Disease
    LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high blood-brain-barrier permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LPA5 antagonist 1
  • HY-12761

    Cannabinoid Receptor Cardiovascular Disease Others Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc .
    A-836339
  • HY-101290

    AAK1 Cyclin G-associated Kinase (GAK) Neurological Disease
    BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain .
    BMT-090605
  • HY-P11642A

    Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor Inflammation/Immunology
    Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
    Sialorphin TFA
  • HY-N9502R

    Reference Standards Endogenous Metabolite Neurological Disease
    Linalool oxide (Standard) is the analytical standard of Linalool oxide (HY-N9502). This product is intended for research and analytical applications. Linalool oxide is a monoterpene and found in aromatic plant essential oils and is a secondary metabolite in elongating wheat plants. Linalool oxide has antinociceptive, anticonvulsant, and anxiolytic activity. Linalool oxide can be used for the research of pain, epilepsy, anxiety disorders .
    Linalool oxide (Standard)
  • HY-174848

    TRP Channel Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease .
    PQM-244
  • HY-149335

    Sigma Receptor Histamine Receptor Neurological Disease
    Sigma-1 receptor antagonist 5 (compound 12),a 4-pyridylpiperidine derivative with analgesic activity,is an antagonist of sigma receptor (Ki=4.5 nM (σ1R),10 nM (σ2R)) and histamine H3 (hH3R,Ki=7.7 nM,IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .
    Sigma-1 receptor antagonist 5
  • HY-180400

    nAChR Calcium Channel Neurological Disease
    PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
    PAM-2
  • HY-181956

    Opioid Receptor Neurological Disease
    MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research .
    MPAM-15
  • HY-182782

    Adenosine Receptor Neurological Disease
    Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid (HY-Y0319)-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases .
    Analgesic agent-4
  • HY-179705

    Opioid Receptor Neurological Disease
    MOR agonist-5 is a selective and potent mu-opioid receptor (MOR) agonist with an EC50 of 0.25 nM. MOR agonist-5 shows an EC50 of 10 nM for DOR and >10000 nM for KOR and NOR. MOR agonist-5 exerts significant antinociceptive activity. MOR agonist-5 can be used for the research of pain .
    MOR agonist-5
  • HY-N17853

    Potassium Channel TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    Siaresinolic acid is a compound found in the leaves of Sabicea grisea. Siaresinolic acid shows antinociceptive and anti-inflammatory activity. Siaresinolic acid reduces nociceptive behavior by ATP-dependent potassium channel, inhibits leukocyte influx, plasma leakage, and proinflammatory mediator (TNF-α, IL-1β) production. Siaresinolic acid does not induce cytotoxicity in murine macrophages, alter locomotor activity at high doses. Siaresinolic acid can be used for the research of pleurisy and pain .
    Siaresinolic acid
  • HY-183673

    COX Neurological Disease Inflammation/Immunology
    COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC50 of 41.6 nM against human COX-1 and an IC50 of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain .
    COX-1/2-IN-12
  • HY-110268

    CXCR Inflammation/Immunology
    NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
    NVP CXCR2 20
  • HY-101290AR

    Cyclin G-associated Kinase (GAK) Reference Standards AAK1 Neurological Disease
    BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
    BMT-090605 hydrochloride (Standard)
  • HY-P11642

    ERK Androgen Receptor Opioid Receptor Enteropeptidase mTOR Aminopeptidase Neurological Disease Inflammation/Immunology Cancer
    Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
    Sialorphin

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