Search Result
Results for "
Antinociceptive
" in MedChemExpress (MCE) Product Catalog:
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108667
-
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P2X Receptor
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Others
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TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats .
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-
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- HY-118785
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-
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- HY-P3870A
-
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Opioid Receptor
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Neurological Disease
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DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
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-
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- HY-N9502
-
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Others
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Neurological Disease
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Linalool oxide is a secondary metabolite in elongating wheat plants with antinociceptive and anticonvulsant effects. Linalool oxide shows anxiolytic activity .
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-
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- HY-N7527
-
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Others
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Neurological Disease
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Baccatin VI is a natural taxoid with antinociceptive activities. Baccatin VI possesses significant antinociceptive activity against p-Benzoquinone-induced abdominal contractions .
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-
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- HY-P3547
-
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Opioid Receptor
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Others
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(D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity .
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-
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- HY-19206
-
-
-
- HY-136623
-
-
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- HY-P3870
-
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Opioid Receptor
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Neurological Disease
|
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DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
|
-
-
- HY-103341
-
-
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- HY-122953
-
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COX
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Inflammation/Immunology
|
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Daturaolone is a natural triterpenoid with anti-inflammatory and antinociceptive potentials. Daturaolone displays a COX-1 inhibitory activity .
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-
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- HY-130432
-
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nAChR
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Neurological Disease
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DBO-83 dihydrochloride is a novel nicotinic acetylcholine receptor agonist, and binds to nAChRs in rat cortical membranes with a Ki value of 4.1 nM. DBO-83 dihydrochloride shows antinociceptive and anti-amnesic activities .
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- HY-151949
-
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Trk Receptor
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Neurological Disease
|
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TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects .
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-
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- HY-131004
-
|
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Cannabinoid Receptor
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Neurological Disease
|
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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 .
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-
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- HY-N0709
-
-
-
- HY-134602
-
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Bacterial
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Inflammation/Immunology
|
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5'-Methoxynobiletin is a potent and orally active antinociceptive and anti-inflammatory agent. 5'-Methoxynobiletin is a polymethoxyflavone, that can be isolated from A. conyzoides .
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-
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- HY-107741
-
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Opioid Receptor
|
Neurological Disease
|
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SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys .
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-
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- HY-N0050
-
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(+)-Allomatrine
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Others
|
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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-
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- HY-W436270
-
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Dopamine Receptor
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Neurological Disease
Inflammation/Immunology
|
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Bulbocapnine hydrochloride, an aporphine alkaloid, is a dopamine receptor inhibitor. Bulbocapnine hydrochloride inhibits dopamine synthesis. Bulbocapnine hydrochloride also has neuroleptic-like, anticonvulsant and antinociceptive effects .
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- HY-113936
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-
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- HY-P1330
-
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P2X Receptor
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Inflammation/Immunology
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Purotoxin 1 is a P2X3 receptor inhibitor. Purotoxin 1 shows antinociceptive properties in animal models of inflammatory pain. Purotoxin 1 can be isolated from the venom of the wolf spider Geolycosa sp .
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-
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- HY-105235
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CI-977
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Opioid Receptor
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Neurological Disease
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Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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-
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- HY-105235A
-
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CI-977 hydrochloride
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Opioid Receptor
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Neurological Disease
|
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Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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-
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- HY-N2772
-
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7-Deoxy-8-epiloganic acid
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Others
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Neurological Disease
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8-Epideoxyloganic acid (7-Deoxy-8-epiloganic acid), an iridoid glucoside, can be found in Incarvillea delavayi. 8-Epideoxyloganic acid exhibits weak antinociceptive activity .
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-
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- HY-N0709R
-
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Bacterial
Fungal
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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Coumarin (Standard) is the analytical standard of Coumarin. This product is intended for research and analytical applications. Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity .
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- HY-B0352B
-
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(R)-Org3770; (R)-6-Azamianserin
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5-HT Receptor
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Neurological Disease
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(R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4 .
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- HY-W015551S
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(E)-Dec-2-enal-d2
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Biochemical Assay Reagents
Isotope-Labeled Compounds
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Others
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trans-2-Decenal-d2 is deuterated labeled Coumarin (HY-N0709). Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity .
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- HY-B0649
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-
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- HY-14316
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Ebanicline; ABT-594
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nAChR
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Neurological Disease
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Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
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-
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- HY-14316C
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Ebanicline tosylate; ABT-594 tosylate
|
nAChR
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Neurological Disease
|
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Tebanicline tosylate, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline tosylate exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
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-
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- HY-N8487
-
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Others
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Neurological Disease
Inflammation/Immunology
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7-Methoxyflavone is a compound isolated from Zornia brasiliensis. 7-Methoxyflavone has peripheral antinociceptive activity. 7-Methoxyflavone inhibits paw-licking time in the neurogenic phase of the formalin pain response (65.6%) and did not decrease the nociceptive response in the inflammatory phase .
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- HY-105294
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Dopamine Receptor
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Others
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FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks .
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- HY-126941
-
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Opioid Receptor
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Neurological Disease
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Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors .
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-
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- HY-100812
-
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GABA Receptor
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Neurological Disease
Endocrinology
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2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats .
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- HY-N9854
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Potassium Channel
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Inflammation/Immunology
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Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitive K + channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects .
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-
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- HY-162552
-
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Opioid Receptor
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Neurological Disease
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KOR/DOR agonist 2 is a KOR and DOR opioid receptors agonist with Ki values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier .
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-
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- HY-P1074
-
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Calcium Channel
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Neurological Disease
|
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SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect .
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- HY-124412
-
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5-HT Receptor
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Neurological Disease
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Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats .
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- HY-101379A
-
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Calcium Channel
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Cardiovascular Disease
Neurological Disease
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8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K + . 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses .
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- HY-14578
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-
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- HY-N0037
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Reactive Oxygen Species
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Inflammation/Immunology
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Albiflorin, a major constituent contained in peony root, is a monoterpene glycoside with neuroprotective effects. Albiflorin also has anti-inflammatory, antioxidant and antinociceptive effects .
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- HY-112692
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Opioid Receptor
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Neurological Disease
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AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
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- HY-112692A
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Opioid Receptor
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Neurological Disease
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AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
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- HY-B0352BS
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(R)-Org3770 d3; (R)-6-Azamianserin d3
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Isotope-Labeled Compounds
5-HT Receptor
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Neurological Disease
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(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
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- HY-W010907
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GPR35
ERK
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Neurological Disease
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Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
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- HY-P1290A
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PKI-(6-22)-amide TFA
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PKA
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Neurological Disease
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PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .
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- HY-P1290
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PKI-(6-22)-amide
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PKA
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Neurological Disease
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PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice .
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- HY-107944
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Maolate; U 19646
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Others
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Neurological Disease
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Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation . Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels . Antinociceptive effect .
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- HY-N0037R
-
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Reactive Oxygen Species
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Inflammation/Immunology
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Albiflorin (Standard) is the analytical standard of Albiflorin. This product is intended for research and analytical applications. Albiflorin, a major constituent contained in peony root, is a monoterpene glycoside with neuroprotective effects. Albiflorin also has anti-inflammatory, antioxidant and antinociceptive effects .
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- HY-N0923
-
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(+)-Corydaline; Corydalin
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Cholinesterase (ChE)
Enterovirus
Opioid Receptor
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Neurological Disease
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Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
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- HY-100714
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DL-AP5
Maximum Cited Publications
18 Publications Verification
2-APV; DL-2-Amino-5-phosphonovaleric acid
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iGluR
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Neurological Disease
Inflammation/Immunology
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DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina .
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- HY-100714C
-
DL-AP5 sodium
Maximum Cited Publications
18 Publications Verification
2-APV sodium; DL-2-Amino-5-phosphonovaleric acid sodium
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iGluR
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Neurological Disease
Inflammation/Immunology
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DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina .
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- HY-107944R
-
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Others
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Neurological Disease
|
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Chlorphenesin carbamate (Standard) is the analytical standard of Chlorphenesin carbamate. This product is intended for research and analytical applications. Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation . Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels . Antinociceptive effect .
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- HY-100714D
-
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2-APV lithium; DL-2-Amino-5-phosphonovaleric acid lithium
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iGluR
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Neurological Disease
Inflammation/Immunology
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DL-AP5 (2-APV) lithium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 lithium shows significantly antinociceptive activity. DL-AP5 lithium specifically blocks on channels in the rabbit retina .
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- HY-N0923R
-
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Cholinesterase (ChE)
Enterovirus
Opioid Receptor
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Neurological Disease
|
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Corydaline (Standard) is the analytical standard of Corydaline. This product is intended for research and analytical applications. Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
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- HY-N0092
-
-
- HY-110150
-
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Others
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Inflammation/Immunology
Cancer
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UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
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- HY-145169
-
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Sodium Channel
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Neurological Disease
|
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AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects .
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- HY-108485
-
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Src
Apoptosis
Fungal
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Infection
Inflammation/Immunology
Cancer
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Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans .
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- HY-108519
-
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ROCK
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Neurological Disease
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AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
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- HY-117702
-
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Prolyl Endopeptidase (PREP)
Aminopeptidase
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Metabolic Disease
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RB 101 is an active mixed inhibitor against two enzymes which metabolize the enkephalins neutral endopeptidase and aminopeptidase N. RB 101 has rather long-lasting antinociceptive effects. RB 101 inhibits the in vivo [ 3H]DPN binding both under basal conditions and after swim stress in mice. RB 101 can be used to determine the precise in vivo localization of enkephalinergic pathways recruited by various stimuli .
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- HY-N0092R
-
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Adenosine Receptor
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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- HY-147907
-
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
|
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Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
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- HY-150028
-
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Cannabinoid Receptor
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Inflammation/Immunology
|
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CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
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- HY-107510
-
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mGluR
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Neurological Disease
|
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YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
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- HY-N0092S3
-
-
- HY-121618
-
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GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
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Infection
Neurological Disease
Cancer
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α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier .
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- HY-147512
-
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Cannabinoid Receptor
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Inflammation/Immunology
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CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis .
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- HY-18099
-
S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
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Neurological Disease
|
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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 .
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- HY-N6648
-
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GABA Receptor
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Neurological Disease
|
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Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
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-
- HY-N13293
-
-
- HY-116143
-
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MAGL
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Metabolic Disease
|
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SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
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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-N0388
-
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Others
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Neurological Disease
|
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Gelsemine, an alkaloid from the Chinese herb Gelsemium elegans, is effective in mitigating chronic pain. Antinociceptive effects.
|
-
- HY-W505771
-
-
- HY-117626
-
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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 .
|
-
- HY-124110
-
|
|
nAChR
|
Neurological Disease
|
|
TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ∗ and α4β2 ∗ nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ∗ nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ∗ nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
|
-
- HY-N0628
-
-
- HY-W031757
-
|
|
Others
|
Inflammation/Immunology
|
|
Anthraquinone-2-carboxylic acid is a major anthraquinone isolated from Brazilian taheebo, with anti-inflammatory activity and antinociceptive .
|
-
- HY-N3990
-
|
(-)-Hardwikiic acid
|
Sodium Channel
|
Infection
Neurological Disease
|
|
Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels. Hardwickiic acid shows insecticidal activity .
|
-
- HY-117979
-
|
Alfadolone
|
GABA Receptor
|
Neurological Disease
|
|
Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia .
|
-
- HY-168352
-
-
- HY-105627A
-
|
CI-572 hydrochloride
|
GABA Receptor
iGluR
|
Cardiovascular Disease
|
|
Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR .
|
-
- HY-78131B
-
|
(R)-Ibuprofen
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-W325509
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
AH 8532, an opioid, possesses anti-nociceptive effect and inhibits writhing induced by phenylquinone, with a ED50 of 16 mg/kg in mice orally .
|
-
- HY-111029
-
|
|
GlyT
|
Neurological Disease
|
|
ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
|
-
- HY-114269
-
|
|
nAChR
|
Neurological Disease
|
|
(-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity .
|
-
- HY-P1795
-
-
- HY-N4109
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity .
|
-
- HY-P3870B
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
|
-
- HY-W109812
-
|
|
COX
|
Inflammation/Immunology
|
|
Sinapyl alcohol is an orally active anti-inflammatory and antinociceptive agent. Sinapyl alcohol reduces the expression level of inducible NO synthase and COX-2 .
|
-
- HY-14223
-
|
|
Others
|
Neurological Disease
|
|
SM-21 is a derivative of R-(+)-hyoscyamine with potent antinociceptive and cognitive enhancing activities. SM-21 works by affecting the release of acetylcholine .
|
-
- HY-P1044
-
|
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
|
-
- HY-N9615
-
-
- HY-P0066
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for the neurotensin receptor. Contulakin G is also a potent antinociceptive agent .
|
-
- HY-111029A
-
|
|
GlyT
|
Others
|
|
ALX-1393 TFA, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
|
-
- HY-P1044A
-
|
LVV-hemorphin-4 TFA
|
Angiotensin Receptor
|
Neurological Disease
|
|
Spinorphin TFA is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
|
-
- HY-171032
-
-
- HY-B2082
-
-
- HY-137988
-
-
- HY-N0388R
-
|
|
Others
|
Neurological Disease
|
|
Gelsemine (Standard) is the analytical standard of Gelsemine. This product is intended for research and analytical applications. Gelsemine, an alkaloid from the Chinese herb Gelsemium elegans, is effective in mitigating chronic pain. Antinociceptive effects.
|
-
- HY-P5795
-
|
|
Sodium Channel
Potassium Channel
|
Neurological Disease
|
|
GsAF-I is a potent Nav and hERG1 channels blocker with IC50s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, Nav1.7 and hERG1, respectively .
|
-
- HY-170444
-
|
|
Histamine Receptor
mAChR
|
Neurological Disease
|
|
ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models .
|
-
- HY-B2114
-
Escin
2 Publications Verification
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Escin, a natural compound of triterpenoid saponins that can be isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent .
|
-
- HY-P6053
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
|
-
- HY-N7144A
-
|
|
Apoptosis
|
Infection
Cancer
|
|
Citronellyl acetate is a monoterpene product of the secondary metabolism of plants, with antinociceptive activity. Citronellyl acetate exhibits pro-apoptotic activity in human hepatoma cells. Citronellyl acetate shows fungicidal, larvicidal, bactericidal and repelling/insecticidal effects .
|
-
- HY-78131BS
-
|
(R)-Ibuprofen-d3
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-B0649S
-
|
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
|
-
- HY-P3499
-
|
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
|
-
- HY-148166
-
|
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
L-Inosine is the L-configuration of Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects .
|
-
- HY-N0628R
-
|
|
Insulin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Kaempferitrin (Standard) is the analytical standard of Kaempferitrin. This product is intended for research and analytical applications. Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.
|
-
- HY-N7126
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway .
|
-
- HY-15028
-
|
ATB-346
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities .
|
-
- HY-P0318
-
-
- HY-Y0892
-
-
- HY-N0746
-
|
|
Others
|
Cancer
|
|
Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides.?Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems . Oxysophocarpine inhibits the?growth?and?metastasis?of ?oral?squamous?cell?carcinoma?(OSCC) .
|
-
- HY-108964
-
|
|
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carvone is a ketone monoterpene found mostly in the essential oils from plants of the genus Mentha. Carvone is widely used in the pharmaceutical industry, cosmetics and agriculture. Carvone has such effects as antimicrobial, antioxidant, anti-inflammatory, antispasmodic, antinociceptive, anticonvulsant .
|
-
- HY-N4109R
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Decursinol (Standard) is the analytical standard of Decursinol. This product is intended for research and analytical applications. Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity .
|
-
- HY-101317A
-
|
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
|
-
- HY-104006
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
|
-
- HY-135408
-
|
|
Drug Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Trimetazidine-N-oxide is the major active metabolite of Trimetazidine. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM. Trimetazidine is an effective antianginal agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties.
|
-
- HY-120813
-
|
URB913
|
Others
|
Inflammation/Immunology
|
|
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA . ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats .
|
-
- HY-B0649R
-
|
2,6-Diisopropylphenol (Standard)
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
|
-
- HY-18978
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions .
|
-
- HY-N2165
-
-
- HY-122219
-
|
|
CCR
|
Inflammation/Immunology
|
|
R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects .
|
-
- HY-W109812S
-
|
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
Sinapyl alcohol-d3 is the deuterated labeled Sinapyl alcohol (HY-W109812). Sinapyl alcohol is an orally active anti-inflammatory and antinociceptive agent. Sinapyl alcohol reduces the expression level of inducible NO synthase and COX-2 .
|
-
- HY-P0185
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
-
- HY-P0185A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
-
- HY-P1319
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
|
-
- HY-P5160
-
|
PhlTx1
|
Sodium Channel
|
Inflammation/Immunology
|
|
Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel .
|
-
- HY-N7144AR
-
|
|
Apoptosis
|
Infection
Cancer
|
|
Citronellyl acetate (Standard) is the analytical standard of Citronellyl acetate. This product is intended for research and analytical applications. Citronellyl acetate is a monoterpene product of the secondary metabolism of plants, with antinociceptive activity. Citronellyl acetate exhibits pro-apoptotic activity in human hepatoma cells. Citronellyl acetate shows fungicidal, larvicidal, bactericidal and repelling/insecticidal effects .
|
-
- HY-N0092S4
-
-
- HY-117506B
-
|
|
FABP
|
Neurological Disease
Inflammation/Immunology
|
|
SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects .
|
-
- HY-168355
-
-
- HY-15249
-
JZL 184
3 Publications Verification
|
MAGL
|
Neurological Disease
|
|
JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH .
|
-
- HY-111539
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research .
|
-
- HY-107690
-
-
- HY-143263
-
|
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-1 (compound SIH 3) is a potent FAAH and MAGL inhibitor with IC50s of 31 nM and 29 nM, respectively. FAAH/MAGL-IN-1 has the potential for the research of neuropathic pain .
|
-
- HY-W008613
-
-
- HY-N8423
-
|
|
ERK
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
α-Amyrin is a pentacyclic triterpenoid compound with oral activity. α-Amyrin activates the ERK and GSK-3β signaling pathways. α-Amyrin can be used in the study of metabolic syndrome induced by high fructose diet and cognitive dysfunction caused by low cholinergic neurotransmission .
|
-
- HY-103528
-
|
Salicylidene salicylhydrazide
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions .
|
-
- HY-162609
-
-
- HY-W008613R
-
|
|
GPR35
ERK
|
Neurological Disease
Inflammation/Immunology
|
|
Pamoic acid (Standard) is the analytical standard of Pamoic acid. This product is intended for research and analytical applications. Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC50 of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties .
|
-
- HY-N8423R
-
|
|
ERK
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
α-Amyrin (Standard) is the analytical standard of α-Amyrin. This product is intended for research and analytical applications. α-Amyrin is a pentacyclic triterpenoid compound with oral activity. α-Amyrin activates the ERK and GSK-3β signaling pathways. α-Amyrin can be used in the study of metabolic syndrome induced by high fructose diet and cognitive dysfunction caused by low cholinergic neurotransmission .
|
-
- HY-19231
-
|
Org 41793
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1319A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
|
-
- HY-N0746R
-
|
|
Others
|
Cancer
|
|
Oxysophocarpine (Standard) is the analytical standard of Oxysophocarpine. This product is intended for research and analytical applications. Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems . Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) .
|
-
- HY-N7126R
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Citronellal (Standard) is the analytical standard of Citronellal. This product is intended for research and analytical applications. Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K? channel pathway .
|
-
- HY-128865
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
|
-
- HY-N0092S1
-
-
- HY-108964R
-
|
|
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carvone (Standard) is the analytical standard of Carvone. This product is intended for research and analytical applications. Carvone is a ketone monoterpene found mostly in the essential oils from plants of the genus Mentha. Carvone is widely used in the pharmaceutical industry, cosmetics and agriculture. Carvone has such effects as antimicrobial, antioxidant, anti-inflammatory, antispasmodic, antinociceptive, anticonvulsant .
|
-
- HY-N6663
-
|
|
COX
|
Inflammation/Immunology
|
|
3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
|
-
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-134189
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
|
-
- HY-135871
-
|
|
AAK1
|
Neurological Disease
|
|
BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
|
-
- HY-147707
-
|
|
Cannabinoid Receptor
|
Others
|
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
|
-
- HY-N5025
-
|
|
P2X Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses . Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed .
|
-
- HY-130605
-
|
|
P2X Receptor
|
Neurological Disease
|
|
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects .
|
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-134189A
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
|
-
- HY-N0092S
-
-
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
-
- HY-101205
-
-
- HY-150721
-
-
- HY-N0092S2
-
-
- HY-Y0892R
-
|
|
Apoptosis
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
4-Hydroxybenzyl alcohol (Standard) is the analytical standard of 4-Hydroxybenzyl alcohol. This product is intended for research and analytical applications. 4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth [4].
|
-
- HY-101100
-
|
D-16949 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Anpirtoline (D-16949) hydrochloride is a centrally acting 5-HT1B receptor agonist, with Kis of 28 nM (5-HT1B), 150 nM (5-HT1A) and 1.49 μM (5-HT2). Anpirtoline hydrochloride has serotonergic, antinociceptive, antidepressant-like effects .
|
-
- HY-101100A
-
|
D-16949
|
5-HT Receptor
|
Neurological Disease
|
|
Anpirtoline (D-16949) is a centrally acting 5-HT1B receptor agonist, with Kis of 28 nM (5-HT1B), 150 nM (5-HT1A) and 1.49 μM (5-HT2). Anpirtoline has serotonergic, antinociceptive, antidepressant-like effects .
|
-
- HY-131914B
-
|
|
Others
|
Inflammation/Immunology
|
|
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
|
-
- HY-B0968
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-100811
-
|
7-CKA
|
iGluR
|
Neurological Disease
|
|
7-Chlorokynurenic acid (7-CKA) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery .
|
-
- HY-100811A
-
|
7-CKA sodium salt
|
iGluR
|
Neurological Disease
|
|
7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid sodium salt is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid sodium salt has potent antinociceptive actions after neuraxial delivery .
|
-
- HY-B0968A
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-101202A
-
|
(Rac)-NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
|
(Rac)-SNC80 is a racemate of SNC80 (HY-101202). SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
|
-
- HY-125527A
-
|
17(R)-RvD1; AT-RvD1
|
TRP Channel
|
Inflammation/Immunology
|
|
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
- HY-B0696A
-
|
NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride
|
GABA Receptor
Trk Receptor
|
Neurological Disease
|
|
Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ∼0.1 μM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties .
|
-
- HY-18618
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-18617
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-145628
-
|
|
Sigma Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
|
-
- HY-N6663R
-
|
|
COX
|
Inflammation/Immunology
|
|
3-Carene (Standard) is the analytical standard of 3-Carene. This product is intended for research and analytical applications. 3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
|
-
- HY-105142
-
|
|
Others
|
Inflammation/Immunology
|
|
M-5011 is a potent and orally active anti-inflammatory agent. M-5011 shows potent antinociceptive effects and inhibits kaolin (HY-W115786)-induced writhing. M-5011 decreases peritoneal 6-keto-PGF1 alpha levels with low ulcerogenic activities. M-5011 shows anti-inflammatory and anti-pyretic effects and analgesic effect .
|
-
- HY-B0968S
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
|
-
- 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 .
|
-
- HY-101202
-
|
NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
|
-
- 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 .
|
-
- HY-161539
-
|
|
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) .
|
-
- HY-B0968S1
-
|
|
Isotope-Labeled Compounds
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine-d9 (dihydrochloride) is deuterium labeled Trimetazidine (dihydrochloride). Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-14840A
-
-
- HY-P1626
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
|
-
- 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 brain 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.
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-B0968R
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine (dihydrochloride) (Standard) is the analytical standard of Trimetazidine (dihydrochloride). This product is intended for research and analytical applications. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-B0968AR
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine (Standard) is the analytical standard of Trimetazidine. This product is intended for research and analytical applications. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-B0380B
-
|
GIC-1001
|
Others
|
Others
|
|
Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
|
-
- HY-159923
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
|
-
- HY-138063
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-136207
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
|
-
- HY-P10358
-
|
|
Calcium Channel
|
Neurological Disease
|
|
TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
|
-
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-N4226
-
|
|
AP-1
|
Inflammation/Immunology
Cancer
|
|
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function .
|
-
- HY-150030
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
|
-
- HY-126052
-
|
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-N2080
-
|
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
|
-
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- 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 .
|
-
- HY-125527AS
-
|
17(R)-RvD1-d5; AT-RvD1-d5
|
Isotope-Labeled Compounds
TRP Channel
|
Inflammation/Immunology
|
|
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
- HY-128971
-
|
|
Cathepsin
Parasite
|
Infection
Neurological Disease
|
|
LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM .
|
-
- HY-N6972
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- HY-162856
-
-
- HY-15026
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
|
-
- HY-N6972R
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3870A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
|
-
- HY-P1074
-
|
|
Calcium Channel
|
Neurological Disease
|
|
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect .
|
-
- HY-P1290A
-
|
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .
|
-
- HY-P0088
-
|
Dynorphin A Porcine Fragment 1-13
|
Opioid Receptor
|
Others
|
|
Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
|
-
- HY-P1795
-
-
- HY-P3547
-
|
|
Opioid Receptor
|
Others
|
|
(D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity .
|
-
- HY-136623
-
-
- HY-P3870
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
|
-
- HY-P1330
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
Purotoxin 1 is a P2X3 receptor inhibitor. Purotoxin 1 shows antinociceptive properties in animal models of inflammatory pain. Purotoxin 1 can be isolated from the venom of the wolf spider Geolycosa sp .
|
-
- HY-P1290
-
|
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice .
|
-
- HY-P3870B
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
|
-
- HY-P0066
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for the neurotensin receptor. Contulakin G is also a potent antinociceptive agent .
|
-
- HY-P1044A
-
|
LVV-hemorphin-4 TFA
|
Angiotensin Receptor
|
Neurological Disease
|
|
Spinorphin TFA is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
|
-
- HY-P5795
-
|
|
Sodium Channel
Potassium Channel
|
Neurological Disease
|
|
GsAF-I is a potent Nav and hERG1 channels blocker with IC50s of 0.36, 0.6, 1.28, 0.33, 1.2, 0.04 and 4.8 μM against Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, Nav1.7 and hERG1, respectively .
|
-
- HY-P6053
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
|
-
- HY-P3499
-
|
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
|
-
- HY-P0318
-
-
- HY-P0185
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
-
- HY-P0185A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
-
- HY-P1319
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
|
-
- HY-P5160
-
|
PhlTx1
|
Sodium Channel
|
Inflammation/Immunology
|
|
Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel .
|
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1319A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
|
-
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
-
- HY-P1626
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-P10358
-
|
|
Calcium Channel
|
Neurological Disease
|
|
TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
|
-
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-108964R
-
-
- HY-N6663
-
-
- HY-N5025
-
-
- HY-Y0892R
-
-
- HY-N6663R
-
|
|
Structural Classification
Other Monoterpenes
other families
Terpenoids
Source classification
Plants
|
COX
|
|
3-Carene (Standard) is the analytical standard of 3-Carene. This product is intended for research and analytical applications. 3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
|
-
- HY-138063
-
-
- HY-N4226
-
|
|
Structural Classification
Microorganisms
other families
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Plants
Disease Research Fields
Cancer
|
AP-1
|
|
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function .
|
-
- HY-126052
-
-
- HY-N2080
-
-
- HY-N6972
-
-
- HY-N6972R
-
|
|
Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-78131BS
-
|
|
|
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
-
- HY-W109812S
-
|
|
|
Sinapyl alcohol-d3 is the deuterated labeled Sinapyl alcohol (HY-W109812). Sinapyl alcohol is an orally active anti-inflammatory and antinociceptive agent. Sinapyl alcohol reduces the expression level of inducible NO synthase and COX-2 .
|
-
-
- HY-N0092S
-
|
|
|
Inosine-2,8-d2 is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .
|
-
-
- HY-N0092S2
-
|
|
|
Inosine- 13C5 is the 13C5 labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .
|
-
-
- HY-W015551S
-
|
|
|
trans-2-Decenal-d2 is deuterated labeled Coumarin (HY-N0709). Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity .
|
-
-
- HY-B0352BS
-
|
|
|
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
|
-
-
- HY-N0092S3
-
|
|
|
Inosine-13C10,15N4 is 13C and 15N labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .
|
-
-
- HY-B0649S
-
|
|
|
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
|
-
-
- HY-N0092S4
-
|
|
|
Inosine-13C3 is a 13C-labeled Inosine that can be used in pharmacokinetic studies of Inosine. Inosine is an agonist of adenosine receptors A1R and A2AR with anti-inflammatory immunomodulatory, antinociceptive and neuroprotective effects .
|
-
-
- HY-N0092S1
-
|
|
|
Inosine- 13C is the 13C labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .
|
-
-
- HY-B0968S
-
|
|
|
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
|
-
-
- HY-B0968S1
-
|
|
|
Trimetazidine-d9 (dihydrochloride) is deuterium labeled Trimetazidine (dihydrochloride). Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
-
- HY-125527AS
-
|
|
|
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-151391
-
|
|
|
Alkynes
|
|
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain 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.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-148166
-
|
|
|
Nucleosides and their Analogs
|
|
L-Inosine is the L-configuration of Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects .
|
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