Search Result
Results for "
Analgesic effect
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108449
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WS-12; AR-15512; AVX-012
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TRP Channel
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Cancer
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Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
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- HY-105808
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- HY-P3445
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- HY-P3445A
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-
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- HY-103344
-
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Aminopeptidase
mGluR
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Neurological Disease
Inflammation/Immunology
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ZJ43 is a potent NAAG peptidase inhibitor, with an IC50 of 2.4 nM and a Ki of 0.8 nM. ZJ43 sufficiently activates group II mGluR and reduces some of the behavioral effects of PCP. ZJ43 shows an analgesic effect in neuropathic and inflammatory and pain models .
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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-149269
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COX
Carbonic Anhydrase
LOX-1
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Inflammation/Immunology
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COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
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- HY-145236
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Others
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Others
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Analgesic agent-1, a potent analgesic agent, shows significant analgesic effect.
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-
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- HY-U00081
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-
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- HY-149274
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Sigma Receptor
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Neurological Disease
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Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance .
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- HY-129668
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Adrenergic Receptor
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Neurological Disease
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Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
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- HY-136720
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Others
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Others
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ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
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- HY-N0398
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Opioid Receptor
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Neurological Disease
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Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect .
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- HY-118756
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RS37326
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Endogenous Metabolite
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Inflammation/Immunology
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Anirolac (RS37326) is a nonsteroidal anti-inflammatory agent with analgesic activity. Anirolac showed analgesic efficacy comparable to that of naproxen in suppressing moderate or severe postpartum uterine pain. Anirolac induced significantly higher analgesia scores than placebo within 6 hours, especially at the 100 mg dose. Anirolac effectively relieved pain and showed a stronger analgesic effect than placebo in every assessment .
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- HY-122323
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Leucylarginine
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Others
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Others
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L-Leucyl-L-arginine (Leucylarginine) is a compound that inhibits the analgesic effect of systemically administered L-arginine in a carrageenan-induced hyperalgesia model in mice when administered intracerebroventricularly.
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- HY-111025
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Others
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Neurological Disease
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Ectylurea,a N-acylurea,can be used in studies of tension and anxiety symptoms, has no effect on the autonomic nervous system, and has no convulsive, analgesic or antispasmodic activity in animals .
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- HY-149498
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- HY-W709349
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D 9998 hydrochloride
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Potassium Channel
iGluR
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Inflammation/Immunology
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Flupirtine hydrochloride (D 9998 hydrochloride) is a selective neuropotassium channel opener with analgesic activity. Flupirtine hydrochloride is used to inhibit a variety of pain conditions, including chronic musculoskeletal pain, migraines, and neuralgia. Flupirtine hydrochloride has antidepressant and antioxidant properties and may increase the analgesic effect in combination therapy with morphine. Flupirtine hydrochloride relieves abnormally increased muscle tension and has a muscle relaxant effect. Flupirtine hydrochloride is clinically superior to other drugs, such as tramadol and pantoxan, plus its side effects are better tolerated. Flupirtine hydrochloride has a significant effect on inhibiting neural hyperexcitability and therefore exhibits inhibitory potential in various pain states .
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- HY-157956
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mAChR
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Neurological Disease
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LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
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- HY-120456
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Opioid Receptor
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Neurological Disease
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SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
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- HY-136644
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Others
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Others
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PD-217014-methyl ester is an α?δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity, and its anti-hyperalgesic effect is dose-dependent.
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- HY-136644A
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Others
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Others
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PD-217014 is an α2δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity reactions. Its anti-allodynic effect is dose-dependent.
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- HY-P0210
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DAMGO
4 Publications Verification
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Opioid Receptor
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Cancer
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DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-P0210B
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Opioid Receptor
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Cancer
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DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-N4219
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Others
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Neurological Disease
Metabolic Disease
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Saikosaponin B3 is a saikosaponin isolated from the roots of Bupleurum falcatum L., with analgesic effect. Saikosaponin B3 inhibits ACTH-induced lipolysis in the fat cells .
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- HY-130118
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- HY-114806
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Flenac; R 67408
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Others
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Inflammation/Immunology
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Fenclofenac is an orally active anti-inflammatory agent with a low ulcerogenic effect. Fenclofenac also exhibits antipyretic and analgesic activities, with an oral LD50 of 2280 mg/kg in rats. Fenclofenac can be utilized in inflammation research .
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- HY-N1965
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Others
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Inflammation/Immunology
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Gaultherin, a natural salicylate derivative, is isolated from Gaultheria yunnanensis. Gaultherin is a non-steroidal anti-inflammatory drug (NSAID). Gaultherin has analgesic and anti-inflammatory effects and lack gastric ulcerogenic effect compared to Aspirin .
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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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- HY-14316C
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Ebanicline tosylate; ABT-594 tosylate
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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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- HY-103567
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mGluR
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Neurological Disease
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Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
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- HY-103567A
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mGluR
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Neurological Disease
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Desmethyl-YM-298198 is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
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- HY-153471
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- HY-P1078
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Calcium Channel
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Neurological Disease
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Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
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- HY-109054
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Drug Metabolite
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Neurological Disease
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O-Demethyltramadol is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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- HY-109054A
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Drug Metabolite
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Neurological Disease
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O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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- HY-P1329
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Opioid Receptor
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Neurological Disease
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CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
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- HY-103506
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NO-711 hydrochloride
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GABA Receptor
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Neurological Disease
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NNC-711 is a potent and selective inhibitor of GAT-1 ( GABA transporter 1) with an IC50 of 40 nM for hGAT-1. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
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- HY-W176629
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-
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- HY-159562
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COX
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Inflammation/Immunology
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COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM) .
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- HY-159561
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COX
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Inflammation/Immunology
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COX-1-IN-2 (compound 5h) is an anti-inflammatory agent with potent analgesic activity. COX-1-IN-2 exhibits a significant inhibitory effect on COX-1 (IC50=38.76 nM) .
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- HY-B0363
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R805
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COX
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Inflammation/Immunology
Cancer
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Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
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- HY-P1078A
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Calcium Channel
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Neurological Disease
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Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
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- HY-N0398R
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Opioid Receptor
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Neurological Disease
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Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect .
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- HY-P1329A
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Opioid Receptor
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Neurological Disease
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CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
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- HY-N7694
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Others
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Inflammation/Immunology
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Isotoosendanin is a limonoid that can be isolated from Melia toosendan fruit. Isotoosendanin displays significant anti-inflammatory and analgesic activities .
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- HY-119820
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SR57746A free base
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5-HT Receptor
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Neurological Disease
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Xaliproden free base is an orally active and selective 5-HT1A receptor agonist. Xaliproden free base shows analgesic effect against acute tonic nociceptive pain and has neuroprotective effects. Xaliproden free base has an acute inhibitory effect on paclitaxel (HY-B0015)-induced mechanical allodynia by inhibiting the excessive response of primary afferent neurons .
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- HY-13222
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Opioid Receptor
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Neurological Disease
Cancer
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BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic .
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- HY-147377
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-
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- HY-159094
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Sodium Channel
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Neurological Disease
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Nav1.8-IN-15 (compound 6) is a potent Nav1.8 inhibitor. Nav1.8-IN-15 shows analgesic effect. Nav1.8-IN-15 has the potential for the research of chronic pain .
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- HY-13913
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NS-398
Maximum Cited Publications
15 Publications Verification
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COX
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Inflammation/Immunology
Cancer
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NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
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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-B0509A
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BAY 41-6551
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Bacterial
Antibiotic
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Infection
Cancer
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Amikacin (BAY 41-6551) is a semisynthetic kanamycin analog that is active against most Gram-negative bacteria, including gentamicin- and tobramycin-resistant strains. Significant inhibitory effect. Amikacin is ototoxic and nephrotoxic. Amikacin can be used in bacteriostatic, anti-cancer and analgesic studies .
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- HY-121679
-
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Others
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Neurological Disease
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COX-2-IN-50 is a water-soluble COX-2 inhibitor with significant analgesic activity. The solubility of COX-2-IN-50 in water reaches 20.3 mg/mL, far exceeding the 1.6 μg/mL of its precursor compound PC407. COX-2-IN-50 demonstrates good biocompatibility and is suitable for the development of injectable dosage forms. COX-2-IN-50 has proven its analgesic effect in vivo and shows potential application value .
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- HY-W013164
-
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COX
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Inflammation/Immunology
Cancer
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SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect .
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- HY-N1965R
-
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Others
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Inflammation/Immunology
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Gaultherin (Standard) is the analytical standard of Gaultherin. This product is intended for research and analytical applications. Gaultherin, a natural salicylate derivative, is isolated from Gaultheria yunnanensis. Gaultherin is a non-steroidal anti-inflammatory drug (NSAID). Gaultherin has analgesic and anti-inflammatory effects and lack gastric ulcerogenic effect compared to Aspirin .
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- HY-90003A
-
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5-HT Receptor
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Neurological Disease
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Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities .
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- HY-90003
-
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5-HT Receptor
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Neurological Disease
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Tianeptine is a selective facilitator of 5-HT uptake. Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine has antidepressant, anxiolytic, analgesic and neuroprotective activities .
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- HY-137451
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S-600918
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P2X Receptor
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Neurological Disease
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Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect .
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- HY-13222A
-
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Opioid Receptor
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Cancer
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BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic .
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- HY-P3223
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Opioid Receptor
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Neurological Disease
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Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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- HY-B0363S
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COX
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Inflammation/Immunology
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Nimesulide-d5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[1][2].
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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- HY-159088
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Opioid Receptor
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Neurological Disease
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KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-B0363R
-
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COX
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Inflammation/Immunology
Cancer
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Nimesulide (Standard) is the analytical standard of Nimesulide. This product is intended for research and analytical applications. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
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- HY-109054AS
-
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Isotope-Labeled Compounds
Drug Metabolite
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Neurological Disease
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O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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- HY-168211
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Epoxide Hydrolase
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Inflammation/Immunology
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LQ-38 is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 5.2 nM. LQ-38 exhibits anti-inflammatory activity in rat foot edema model and mouse acute pancreatitis model, exhibits analgesic effect in Acetic acid (HY-Y0319)-induced writhing mouse model .
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- HY-138232
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LTNAM
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Others
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Neurological Disease
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Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
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- HY-116275
-
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Others
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Cancer
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KRM-II-81 is a gamma-aminobutyric acid type A (GABAA) receptor ligand with analgesic, anxiolytic and anti-epileptic activities. KRM-II-81 exhibits positive allosteric modulation of GABAA receptors selective for the α2/3 subunit. KRM-II-81 reduces formalin-induced pain response after oral administration. KRM-II-81 significantly reduces pain behavior induced by chronic spinal nerve ligation. Analysis of KRM-II-81 showed that its plasma and brain concentrations were positively correlated with analgesic effects. The enhancement effect of KRM-II-81 on GABA current shows its key role in the analgesic mechanism. KRM-II-81 was less effective in respiratory depression, demonstrating its safety and tolerability .
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- HY-138257A
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AS1069562; (R)-YM-08054 benzenesulfonate
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5-HT Receptor
Serotonin Transporter
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Neurological Disease
Metabolic Disease
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(R)-Indeloxazine benzenesulfonate (AS1069562) is an orally active 5-HT and NE reuptake inhibitor, with IC50 values of 0.35 μM and 3.3 μM, respectively. (R)-Indeloxazine benzenesulfonate (AS1069562) possesses curative-like analgesic effect. (R)-Indeloxazine benzenesulfonate (AS1069562) might improve nerve function impairment via the amelioration of neurotrophic support .
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- HY-132428S
-
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
|
O-Desmethyl Tramadol-d6 is the deuterium labeled O-Desmethyl Tramadol. O-Desmethyl Tramadol is a primary active metabolite of Tramadol. O-Desmethyl Tramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme[1].
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- HY-W013712
-
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Potassium Channel
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Neurological Disease
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GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
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- HY-B0985A
-
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TRP Channel
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Neurological Disease
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Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
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- HY-90003AR
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5-HT Receptor
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Neurological Disease
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Tianeptine (sodium salt) (Standard) is the analytical standard of Tianeptine (sodium salt). This product is intended for research and analytical applications. Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities .
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- HY-12811
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Sodium Channel
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Neurological Disease
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PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
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- HY-138257
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(S)-AS1069562; (S)-YM-08054 benzenesulfonate
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5-HT Receptor
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Neurological Disease
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(S)-AS1069562 is the S-enantiomer of AS1069562 (HY-138257A). AS1069562 is an orally active 5-HT and NE reuptake inhibitor, with IC50 values of 0.35 μM and 3.3 μM, respectively. AS1069562 possesses curative-like analgesic effect. AS1069562 might improve nerve function impairment via the amelioration of neurotrophic support .
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- HY-B0985
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TRP Channel
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Neurological Disease
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Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
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- HY-105142
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Others
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Inflammation/Immunology
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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 .
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- HY-15036B
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DDNL
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Others
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Inflammation/Immunology
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Diclofenac deanol (DDNL) is a nonsteroidal anti-inflammatory drug with anti-inflammatory, analgesic and antipyretic activities. Diclofenac deanol has a more potent inhibitory effect on cyclooxygenase (COX)-2 than on COX-1. The solubility of diclofenac deanol is significantly higher than that of other diflunisal salts reported earlier. Diclofenac deanol has a wide range of potential applications in the medical field due to its biological activity and high water solubility .
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- HY-100813
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GABA Receptor
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Neurological Disease
Inflammation/Immunology
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Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats .
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- HY-115861
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Others
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Neurological Disease
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UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies .
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- HY-B0985R
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TRP Channel
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Neurological Disease
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Phenazopyridine (hydrochloride) (Standard) is the analytical standard of Phenazopyridine (hydrochloride). This product is intended for research and analytical applications. Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
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- HY-N7934
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(-)-Trachelogenin
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HCV
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Infection
Neurological Disease
Inflammation/Immunology
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Trachelogenin ((-)-Trachelogenin) is an HCV entry inhibitor without genotype specificity, and with low cytotoxicity. Trachelogenin inhibits HCVcc infection and HCVpp cell entry in a dose-dependent manner with an IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively. Trachelogenin exhibits effective antiviral, anti-inflammatory and analgesic effects .
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- HY-111011
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JNJ 38488502 acetate; FE 200665 acetate
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Others
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Neurological Disease
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CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
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- HY-19500
-
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Others
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Others
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SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
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- HY-14909
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Bardoxolone
Maximum Cited Publications
15 Publications Verification
CDDO; RTA 401
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Keap1-Nrf2
Necroptosis
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Metabolic Disease
Cancer
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Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease .
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- HY-P5865
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Theraphotoxin-Tap1a; TRTX-Tap1a; µ/ω-TRTX-Tap1a
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Sodium Channel
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Neurological Disease
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Tap1a (Theraphotoxin-Tap1a) is a spider venom peptide that inhibits sodium channels with IC50s of 80 nM and 301 nM against Nav1.7 and Nav1.1, respectively. Tap1a shows analgesic effects .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0210
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DAMGO
4 Publications Verification
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Opioid Receptor
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Cancer
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DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-P0210B
-
|
Opioid Receptor
|
Cancer
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DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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-
- HY-P3445
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-
- HY-P3445A
-
-
- HY-P1617
-
|
Peptides
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Neurological Disease
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LY 190388 is a penicillamine-containing enkefa peptide analog with μ receptor agonist activity. LY 190388 showed analgesic effect in inhibiting the writhing response in mice after intracerebroventricular administration. The analgesic effect of LY 190388 is not caused by its δ receptor agonist action, but by its μ receptor agonist activity. When LY 190388 is used together with the δ receptor antagonist ICI 174864, an additive analgesic effect is produced .
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-
- HY-P0007
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Carbocalcitonin
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Peptides
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Metabolic Disease
|
Elcatonin (Carbocalcitonin) is a synthetic analog of eel calcitonin. Elcatonin increases bone mineral density, inhibits bone resorption and processes a central analgesic effect .
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-
- HY-P1078
-
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Calcium Channel
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Neurological Disease
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Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
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-
- HY-P1329
-
|
Opioid Receptor
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Neurological Disease
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
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- HY-P1078A
-
|
Calcium Channel
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Neurological Disease
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Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels .
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-
- HY-P3549
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|
Peptides
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Neurological Disease
|
[D-Ala2] Leu-Enkephalinamide is an enkephalin analog. [D-Ala2] Leu-Enkephalinamide has great corneal permeability and analgesic effect. [D-Ala2] Leu-Enkephalinamide can be used for the research of ocular diseases .
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-
- HY-P1329A
-
|
Opioid Receptor
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Neurological Disease
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
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- HY-P3223
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|
Opioid Receptor
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Neurological Disease
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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-
- HY-P3869
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|
Peptides
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Neurological Disease
|
[D-Arg2]Dermorphin-(1-4) amide is a N-terminal shorter peptide amide of [D-Arg2]dermorphin with the hypothermic effect. [D-Arg2]Dermorphin-(1-4) amide shows analgesic activity and degradation in soluble mouse liver and brain extracts .
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-
- HY-P10203
-
|
Opioid Receptor
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Inflammation/Immunology
|
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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-
- HY-P5865
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Theraphotoxin-Tap1a; TRTX-Tap1a; µ/ω-TRTX-Tap1a
|
Sodium Channel
|
Neurological Disease
|
Tap1a (Theraphotoxin-Tap1a) is a spider venom peptide that inhibits sodium channels with IC50s of 80 nM and 301 nM against Nav1.7 and Nav1.1, respectively. Tap1a shows analgesic effects .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0363S
-
|
Nimesulide-d5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[1][2].
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-
-
- HY-109054AS
-
|
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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-
-
- HY-132428S
-
|
O-Desmethyl Tramadol-d6 is the deuterium labeled O-Desmethyl Tramadol. O-Desmethyl Tramadol is a primary active metabolite of Tramadol. O-Desmethyl Tramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme[1].
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Cat. No. |
Product Name |
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Classification |
-
- HY-159562
-
|
|
Azide
|
COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM) .
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- HY-159561
-
|
|
Azide
|
COX-1-IN-2 (compound 5h) is an anti-inflammatory agent with potent analgesic activity. COX-1-IN-2 exhibits a significant inhibitory effect on COX-1 (IC50=38.76 nM) .
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