Search Result
Results for "
Analgesic effect
" in MedChemExpress (MCE) Product Catalog:
9
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0509A
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Amikacin
Maximum Cited Publications
26 Publications Verification
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-P0210
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DAMGO
Maximum Cited Publications
12 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-108449
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WS-12; AR-15512; AVX-012
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TRP Channel
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Neurological Disease
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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-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-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-13913
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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-N3017
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Antibiotic
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Neurological Disease
Inflammation/Immunology
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Artemitin is a flavonoid neuroanesthetic agent with moderate cytotoxicity. Artemitint has selective inhibitory activity against Meth-A sarcoma cells with an ED50 of 5-10 μg/mL, and has no significant effect on LLC lung cancer cells. Artemitin exerts anticancer activity by affecting cell proliferation signaling pathways, and also has potential anti-inflammatory and neuroprotective effects. Artemitin exhibits a dose-dependent antinociceptive effect in the mouse hot plate test, with an ED50 of 1.6 μg/kg, and has analgesic activity .
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- HY-N8290
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-
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- HY-N8487
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Cytochrome P450
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Neurological Disease
Inflammation/Immunology
Cancer
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7-Methoxyflavone is a flavonoid compound that can be isolated from Zornia brasiliensis. 7-Methoxyflavone can bind to human serum albumin and is an aromatase inhibitor. 7-Methoxyflavone has peripheral analgesic and certain antitumor activities. 7-Methoxyflavone is effective against chemical pain but has no significant effect on thermal pain .
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- HY-P3445A
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-
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- HY-W013331
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2-Deoxyartemisinin
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TNF Receptor
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Neurological Disease
Inflammation/Immunology
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Deoxyartemisinin (2-Deoxyartemisinin) is an orally active anti-inflammatory and analgesic agent. Deoxyartemisinin selectively reduces the level of the pro-inflammatory cytokine TNF-α. Deoxyartemisinin alleviates neuropathic pain, inflammatory pain, and croton oil-induced ear edema.\nDeoxyartemisinin exerts an analgesic effect against thermal stimulation. Deoxyartemisinin has anti-ulcer activity. Deoxyartemisinin can be used in research related to inflammatory diseases, pain, and gastric ulcers .
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- HY-17391
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Adenosine Receptor
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Endocrinology
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Pamabrom is a diuretic that acts on the opioid receptor-nitric oxide (NO) -cyclic guanosine monophosphate (cGMP) -K + channel pathway. Pamabrom exerts peripheral antinociceptive activity by activating this pathway. The mechanism involves activating opioid receptors, promoting the release of nitric oxide, and then influencing cyclic guanosine monophosphate and K channels to produce an analgesic effect. Pamabrom is orally active and is mainly used in the research and treatment of premenstrual syndrome and primary dysmenorrhea[1].
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- HY-P3445
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- HY-P0210B
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DAMGO TFA
Maximum Cited Publications
12 Publications Verification
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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-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-109054A
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Drug Metabolite
Opioid Receptor
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Neurological Disease
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O-Desmethyltramadol hydrochloride is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol hydrochloride mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR) .
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- HY-W176629
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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-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-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-W050088
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HP 549
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Drug Derivative
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Neurological Disease
Inflammation/Immunology
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Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
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- HY-109054
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Drug Metabolite
Opioid Receptor
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Neurological Disease
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O-Desmethyltramadol is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR) .
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- HY-114806
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Flenac; R 67408
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Thyroid Hormone Receptor
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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-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-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-178494
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Sodium Channel
Potassium Channel
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Neurological Disease
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Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC50 of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease .
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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-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-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-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-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-105808
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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-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-108449S
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WS-12-d3; AR-15512-d3; AVX-012-d3
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Isotope-Labeled Compounds
TRP Channel
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Neurological Disease
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Acoltremon-d3 (WS-12-d3) is the deuterium labeled Acoltremon (HY-108449). Acoltremon 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-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-P1617
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Endogenous Metabolite
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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-136720
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COX
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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-171758
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Opioid Receptor
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Neurological Disease
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BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC50 values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence .
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- HY-P0007
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Carbocalcitonin
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Drug Intermediate
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Metabolic Disease
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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-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-153471
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- HY-N11960
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Opioid Receptor
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Inflammation/Immunology
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Ignavine is a conformational modulator of μ-opioid receptors (IC50 = 2.0 μM). Ignavine exhibits a concentration dependent bidirectional regulatory effect in vitro. Ignavine has analgesic activity. Ignavine can be used for research on pain related conditions .
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- HY-173016
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Opioid Receptor
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Neurological Disease
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HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
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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-109054AS
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Isotope-Labeled Compounds
Drug Metabolite
Opioid Receptor
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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 the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol hydrochloride mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR) .
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- HY-P3223A
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Opioid Receptor
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Neurological Disease
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Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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- HY-W013164R
-
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Reference Standards
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-N8290R
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Lactucopicrin (Standard)
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Autophagy
NF-κB
AMPK
Reference Standards
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Neurological Disease
Metabolic Disease
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Lactupicrin (Standard) is the analytical standard of Lactupicrin. This product is intended for research and analytical applications. Lactupicrin (Lactucopicrin) exhibits analgesic, sedative, antimalarial activities and atheroprotective effect. Lactupicrin inhibits acetylcholinesterase (AChE) with an IC50 of 150.3 μM. Lactupicrin is an orally active characteristic bitter sesquiterpene lactone .
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- HY-P991622
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Trk Receptor
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Neurological Disease
Inflammation/Immunology
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MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain .
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- HY-132428S
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Isotope-Labeled Compounds
Opioid Receptor
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Neurological Disease
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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 .
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- HY-106601A
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LY-150720 hydrochloride
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Opioid Receptor
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Neurological Disease
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Picenadol (LY-150720) hydrochloride is an opioid mixed agonist-antagonist analgesic. Picenadol hydrochloride is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol hydrochloride has anticholinergic activity .
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- HY-172774
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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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- HY-U00081
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- HY-W326260
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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-122323
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Leucylarginine
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Amino Acid Derivatives
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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-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-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-149498
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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-136644
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Calcium Channel
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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-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-136644A
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Calcium Channel
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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-105808R
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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-138839
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Opioid Receptor
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Neurological Disease
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Allyphenyline oxalate (compound 9) can enhance the analgesic effect of Morphine. The pKi values of Allyphenyline for α2A, α2B and α2C are 7.24, 6.47 and 7.07, respectively .
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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-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-N0398R
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Reference Standards
Opioid Receptor
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Neurological Disease
|
|
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-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-147377
-
-
- HY-114806R
-
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Flenac (Standard); R 67408 (Standard)
|
Thyroid Hormone Receptor
Reference Standards
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Inflammation/Immunology
|
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Fenclofenac (Standard) is the analytical standard of Fenclofenac. This product is intended for research and analytical applications. 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-121679
-
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COX
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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-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
|
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-B0363S
-
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|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
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 .
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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-P10203
-
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|
Opioid Receptor
|
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-B0363R
-
|
R805 (Standard)
|
Reference Standards
COX
|
Inflammation/Immunology
Cancer
|
|
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-168211
-
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Epoxide Hydrolase
|
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
|
Aminopeptidase
|
Neurological Disease
|
|
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-138257A
-
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AS1069562; (R)-YM-08054 benzenesulfonate
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
(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-B0363S1
-
|
R805-13C6
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
Cancer
|
|
Nimesulide- 13C6 (R805- 13C6) is 13C 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.
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-
- HY-138257
-
|
(S)-AS1069562; (S)-YM-08054 benzenesulfonate
|
5-HT Receptor
|
Neurological Disease
|
|
(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-106601
-
|
LY-150720
|
Opioid Receptor
|
Neurological Disease
|
|
Picenadol (LY-150720) is an opioid mixed agonist-antagonist analgesic. Picenadol is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol has anticholinergic activity .
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-
- HY-13913R
-
|
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COX
|
Inflammation/Immunology
Cancer
|
|
NS-398 (Standard) is the analytical standard of NS-398. This product is intended for research and analytical applications. 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-108449R
-
|
WS-12 (Standard); AR-15512 (Standard); AVX-012 (Standard)
|
Reference Standards
TRP Channel
|
Neurological Disease
|
|
Acoltremon (Standard) is the analytical standard of Acoltremon (HY-108449). This product is intended for research and analytical applications. 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-165374
-
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Others
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Inflammation/Immunology
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|
AY-30068 is an orally effective analgesic. AY-30068 exists in the enterohepatic circulation and has a long-lasting analgesic effect .
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-
- HY-105977
-
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Others
|
Inflammation/Immunology
|
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Chinoin 127 is a non anesthetic analgesic agent with strong anti-inflammatory activity. Chinoin 127 shows potent analgesic effect in the hot plate test, Randall Selitto test, and torsion test .
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-
- HY-118756
-
|
RS37326
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
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-105525
-
|
NIH 10908 free base
|
Opioid Receptor
|
Neurological Disease
|
|
Sameridine (NIH-10908 free base) is a weak partial agonist of the μ-opioid receptor. Sameridine shows local anesthetic and analgesic properties. Sameridine has minimal respiratory depression at low doses, but can suppress ventilatory response at high doses. Sameridine can be used for the study of analgesic effect .
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-
- HY-105389
-
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RWJ-38705
|
Opioid Receptor
|
Neurological Disease
|
|
Tramadol N-oxide (RWJ 38705) is an analgesic. Tramadol N-oxide sproduces dose-related, long-lasting antinociception. Tramadol N-oxide has affinity for μ opioid receptor (Ki = 38.5 μM) and δ, κ receptors (Ki > 100 μM). Tramadol N-oxide can be used for the study of analgesic effect .
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- HY-P11480
-
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Trk Receptor
|
Neurological Disease
|
|
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF (IC50: 21 nM for human TrkA in PathHunter assay). TrkA/NGF-IN-1 shows an analgesic effect in a rat incisional pain model .
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-
- HY-119348
-
|
NCX-701
|
Interleukin Related
TNF Receptor
COX
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
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Nitroparacetamol (NCX-701) is a nitric oxide (NO) donor-non-steroidal anti-inflammatory agent (NO-NSAID). Nitroparacetamol is formed by the ester linkage of Acetaminophen (HY-66005) and Nitrooxybutyroyl, aiming to combine the analgesic advantage of Acetaminophen with the organ-protective effect of nitric oxide, while expanding its anti-inflammatory activity. The analgesic spectrum of Nitroparacetamol is broader, and it is effective for painful pathological pain, and significantly reduces hepatotoxicity. Nitroparacetamol can reduce the expressions of IL-1β, TNF-α, COX-2, and iNOS.
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- HY-148605
-
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ATP Synthase
Drug Derivative
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Aloracetam is a γ-aminobutyric acid cyclic derivative that can pass through the blood-brain barrier and has a significant enhancing cognitive function effect. Aloracetam improves the blood perfusion of brain tissue, increases the synthesis of proteins, ATP and acetylcholine in the brain, enhances the excitatory conduction effect of cholinergic nerves, and reduces the damage to brain tissue caused by cerebral vascular diseases. Aloracetam also has certain anti-epileptic, anti-inflammatory, analgesic and anti-depressant effects .
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- HY-108519R
-
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|
Reference Standards
ROCK
|
Neurological Disease
|
|
AS1892802 (Standard) is the analytical standard of AS1892802 (HY-108519). This product is intended for research and analytical applications. 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-182584
-
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5-HT Receptor
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Neurological Disease
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|
S 15931 is a 5-HT1A receptor inhibitor. S 15931 inhibits the late-phase hindpaw licking response induced by formalin and the abdominal writhing response induced by acetic acid in Mus musculus. S 15931 abolishes the spontaneous tail-flick response induced by 8-OH-DPAT in Rattus norvegicus and potentiates the analgesic effect of morphine. S 15931 is applicable for pain-related research .
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-
- HY-N16538
-
|
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Drug Derivative
|
Cardiovascular Disease
Neurological Disease
|
|
4-(Acetoxymethyl)phenyl glucoside is a type of gastrodin derivative that can cross the blood-brain barrier. 4-(Acetoxymethyl)phenyl glucoside exhibits sedative, anticonvulsant and analgesic effects in mouse models. 4-(Acetoxymethyl)phenyl glucoside can be used for research on senile cardiovascular and cerebrovascular diseases as well as brain nerve disorders .
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-
- HY-178235
-
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Opioid Receptor
|
Neurological Disease
|
|
MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .
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-
- HY-15036B
-
|
DDNL
|
COX
|
Inflammation/Immunology
|
|
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-P1241A
-
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|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) TFA induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) TFA has an analgesic effect and can also inhibit the activation of microglia .
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-
- HY-P1241
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22), a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) has an analgesic effect and can also inhibit the activation of microglia .
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-
- HY-105142
-
|
|
COX
|
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-115861
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
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-P5865
-
|
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 .
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-
- HY-B0985R
-
|
|
Reference Standards
TRP Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-W050088S
-
|
HP 549-d6
|
Isotope-Labeled Compounds
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
|
|
Isoxepac-d6 (HP 549-d6) is the deuterium labeled Isoxepac (HY-W050088). Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
|
-
- HY-N8487R
-
|
|
Reference Standards
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
7-Methoxyflavone (Standard) is the analytical standard of 7-Methoxyflavone (HY-N8487). This product is intended for research and analytical applications. 7-Methoxyflavone is a flavonoid compound that can be isolated from Zornia brasiliensis. 7-Methoxyflavone can bind to human serum albumin and is an aromatase inhibitor. 7-Methoxyflavone has peripheral analgesic and certain antitumor activities. 7-Methoxyflavone is effective against chemical pain but has no significant effect on thermal pain .
|
-
- HY-115500
-
|
|
Endogenous Metabolite
Opioid Receptor
Leukotriene Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4). PL265 can be used in non-addictive chronic pain research .
|
-
- HY-N18124
-
|
|
Others
|
Neurological Disease
|
|
1-O-Tigloyl-1-O-debenzoylohchinal is an orally active limonoid-type triterpenoid anti-inflammatory and peripheral analgesic agent isolated from the fruits of Melia toosendan. 1-O-Tigloyl-1-O-debenzoylohchinal significantly inhibits acetic acid (HY-Y0319)-induced increase in vascular permeability, λ-Carrageenan (HY-N9470)-induced paw edema, and acetic acid-induced writhing response in mice. 1-O-Tigloyl-1-O-debenzoylohchinal shows no significant analgesic effect in the hot-plate test, and acts mainly on the peripheral rather than the central nervous system. 1-O-Tigloyl-1-O-debenzoylohchinal can be widely used in the research of acute or chronic inflammation, stomachache and other related diseases .
|
-
- HY-111011
-
|
JNJ 38488502 acetate; FE 200665 acetate
|
Opioid Receptor
|
Neurological Disease
|
|
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-B2185
-
|
|
Dopamine Receptor
Potassium Channel
AMPK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Tipepidine citrate is a non-narcotic antitussive agent. Tipepidine citrate reversibly inhibits dopamine D2 receptor-mediated GIRK current (IDA(GIRK)), thereby activating VTA dopamine neurons, with an IC50 of 7.0 μM for IDA(GIRK). Tipepidine activates AMPK. Tipepidine citrate has antidepressant-like effects. Tipepidine citrate enhances the analgesic effect of Carbamazepine (HY-B0246). Tipepidine citrate improves adipose tissue fibrosis and glucose intolerance in high-fat diet-induced obese mice .
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-
- HY-W050088R
-
|
HP 549 (Standard)
|
Reference Standards
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
|
|
Isoxepac (Standard) (HP 549 (Standard)) is the analytical standard of Isoxepac (HY-W050088). This product is intended for research and analytical applications. Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
|
-
- HY-103506
-
|
NO-711 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
|
-
- HY-111664
-
|
(+)-Citronellal
|
Bacterial
Fungal
Insecticide
Taste Receptor
Opioid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
(R)-(+)-Citronellal ((+)-Citronellal) is a monoterpenoid compound and is one of the main components of essential oils from plants such as lemon grass. (R)-(+)-Citronellal has antibacterial, antifungal, and insecticidal activities. (R)-(+)-Citronellal alleviates the bitterness of caffeine by antagonizing the bitter taste receptors Tas2r43 (IC50 = 84 μM) and Tas2R46. (R)-(+)-Citronellal generates analgesic activity by activating the opioid receptor (broad-spectrum opioid receptor) pathway, and its effect is particularly significant for inflammatory pain .
|
-
- HY-19500
-
|
|
COX
|
Others
|
|
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.
|
-
- HY-121554
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Kojic amine is an orally active γ-aminobutyric acid (GABA) analog. Kojic amine acts as a GABA mimic that inhibits sodium-independent [ 3H]GABA binding to rat brain cell membranes. Kojic amine reduces flexor spasms in chronic spinal rat and cat models. Kojic amine prevents tonic extensor convulsions in mice. Kojic amine produces a transient, dose-dependent analgesic effect in the mouse hot-plate test. Kojic amine can be used in research related to skeletal muscle spasm, epilepsy and analgesia [1][2]
|
-
- HY-145453
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress .
|
-
- HY-W583729
-
|
|
Biochemical Assay Reagents
|
Others
|
|
DL-Poly (lactic acid) is a biodegradable poly (α-hydroxy acid) matrix and a coating material for controlled drug release. DL-Poly (lactic acid) is classified as a drug release retardant, which degrades into natural lactic acid monomers, an intermediate product of carbohydrate metabolism, enabling complete drug delivery that lasts for several weeks. Its drug release rate is affected by the pH of the surrounding environment .
|
-
- HY-103506R
-
|
NO-711 hydrochloride (Standard)
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
|
NNC-711 (Standard) is the analytical standard of NNC-711 (HY-103506). This product is intended for research and analytical applications. NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
|
-
- HY-145453R
-
|
|
Reference Standards
Interleukin Related
|
Inflammation/Immunology
|
|
Propacetamol (Standard) is the analytical standard of Propacetamol (HY-145453). This product is intended for research and analytical applications. Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress .
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-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-110036
-
|
L768242
|
Cannabinoid Receptor
Endogenous Metabolite
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
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-
- HY-101392A
-
|
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-110036A
-
|
L768242 hydrochloride
|
Cannabinoid Receptor
Endogenous Metabolite
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
|
-
- HY-178281
-
|
|
Potassium Channel
Sodium Channel
|
Neurological Disease
|
|
E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
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-
- HY-N0885
-
|
Telobufotoxin; Telocinobufogenin
|
JAK
STAT
mTOR
PI3K
Akt
Polo-like Kinase (PLK)
Na+/K+ ATPase
Apoptosis
Bacterial
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na +/K +-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models .
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-
- HY-N0346
-
|
Ethyl p-methoxycinnamate
|
COX
NF-κB
TNF Receptor
Interleukin Related
Apoptosis
VEGFR
Bacterial
Dengue Virus
Caspase
|
Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC50 = 1.12 μM) and COX-2 (IC50 = 0.83 μM)), NF-κB (IC50 = 88.7 μM) and cytokine production (TNF-α (IC50 = 96.84 μg/mL) and IL-1β (IC50 = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats .
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-
- HY-W700834
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
|
|
Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-W777360
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
Monoamine Oxidase
nAChR
Opioid Receptor
Imidazoline Receptor
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-145491
-
|
|
ERK
NF-κB
CCR
|
Inflammation/Immunology
|
|
Resolvin D5 is an anti-inflammatory and analgesic agent produced in M2 macrophages. Resolvin D5 alleviates Paclitaxel (HY-B0015)-induced mechanical allodynia and inflammatory pain by activating the GPR32 receptor, with gender specificity (effective only in male mice) and independence from TRPV1 or TRPA1 channels. Resolvin D5 attenuates LPS-induced ERK phosphorylation and NF-κB nuclear translocation, downregulates proinflammatory mediators such as IL-6 and CCL5, inhibits Th17 cell differentiation and osteoclastogenesis, promotes regulatory T cell differentiation, and shows no cytotoxicity to human monocytes. The level of Resolvin D5 is elevated in arthritic SKG mice, but Resolvin D5 has no effect on dendritic cell differentiation or M1 macrophage polarization, nor does it prevent ZyA-induced arthritis progression. Resolvin D5 is suitable for research related to chemotherapy-induced peripheral neuropathy, inflammatory pain and rheumatoid arthritis .
|
-
- HY-N4267
-
|
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
|
-
- HY-B0527
-
|
|
Serotonin Transporter
Trk Receptor
Sodium Channel
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
mAChR
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
- HY-B0527A
-
|
|
Serotonin Transporter
5-HT Receptor
mAChR
Histamine Receptor
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
- HY-B0527AS
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
- HY-B0527AR
-
|
|
Reference Standards
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0210
-
DAMGO
Maximum Cited Publications
12 Publications Verification
|
Opioid Receptor
|
Cancer
|
|
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-P1241
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22), a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) has an analgesic effect and can also inhibit the activation of microglia .
|
-
- HY-P3445A
-
-
- HY-P3445
-
-
- HY-P0210B
-
DAMGO TFA
Maximum Cited Publications
12 Publications Verification
|
Opioid Receptor
|
Cancer
|
|
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
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 .
|
-
- HY-P3869
-
|
[D-Arg2]Dermorphin-(1-4) amide
|
Peptides
|
Neurological Disease
|
|
Lumekefamide ([D-Arg2]Dermorphin-(1-4) amide) is a N-terminal shorter peptide amide of [D-Arg2]dermorphin with the hypothermic effect. Lumekefamide shows analgesic activity and degradation in soluble mouse liver and brain extracts .
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
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 .
|
-
- HY-P1617
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
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 .
|
-
- HY-P0007
-
|
Carbocalcitonin
|
Drug Intermediate
|
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 .
|
-
- HY-P3223A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-P1078
-
|
|
Calcium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-P1078A
-
|
|
Calcium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-P3223
-
|
|
Opioid Receptor
|
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 .
|
-
- HY-P10203
-
|
|
Opioid Receptor
|
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 .
|
-
- HY-P1241A
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) TFA induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) TFA has an analgesic effect and can also inhibit the activation of microglia .
|
-
- HY-P5865
-
|
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 .
|
-
- HY-P11480
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF (IC50: 21 nM for human TrkA in PathHunter assay). TrkA/NGF-IN-1 shows an analgesic effect in a rat incisional pain model .
|
-
- HY-P3549
-
|
|
Peptides
|
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 .
|
-
- HY-P3869A
-
|
[D-Arg2]Dermorphin-(1-4) amide TFA
|
Peptides
|
Neurological Disease
|
|
Lumekefamide TFA ([D-Arg2]Dermorphin-(1-4) amide TFA) is a N-terminal shorter peptide amide of [D-Arg2]dermorphin with the hypothermic effect. Lumekefamide shows analgesic activity and degradation in soluble mouse liver and brain extracts .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991622
-
|
|
Trk Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-101392
-
Harmane
1 Publications Verification
|
Alkaloids
other families
Pyridine Alkaloids
Plants
Indole Alkaloids
Source Classification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-N3017
-
-
-
- HY-N8290
-
-
-
- HY-N8487
-
-
-
- HY-111664
-
-
-
- HY-N0398
-
-
-
- HY-101392A
-
|
|
Apocynaceae
Alkaloids
Other Alkaloids
Plants
Rauwolfia canescens
Source Classification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-N0885
-
-
-
- HY-145491
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
ERK
NF-κB
CCR
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Resolvin D5 is an anti-inflammatory and analgesic agent produced in M2 macrophages. Resolvin D5 alleviates Paclitaxel (HY-B0015)-induced mechanical allodynia and inflammatory pain by activating the GPR32 receptor, with gender specificity (effective only in male mice) and independence from TRPV1 or TRPA1 channels. Resolvin D5 attenuates LPS-induced ERK phosphorylation and NF-κB nuclear translocation, downregulates proinflammatory mediators such as IL-6 and CCL5, inhibits Th17 cell differentiation and osteoclastogenesis, promotes regulatory T cell differentiation, and shows no cytotoxicity to human monocytes. The level of Resolvin D5 is elevated in arthritic SKG mice, but Resolvin D5 has no effect on dendritic cell differentiation or M1 macrophage polarization, nor does it prevent ZyA-induced arthritis progression. Resolvin D5 is suitable for research related to chemotherapy-induced peripheral neuropathy, inflammatory pain and rheumatoid arthritis .
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- HY-N4267
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Cardiovascular Disease
Structural Classification
other families
Classification of Application Fields
Lignans
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
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Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
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Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
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- HY-N7934
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- HY-N0346
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Ethyl p-methoxycinnamate
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Structural Classification
Kaempferia galanga L.
Iridoids
Terpenoids
Plants
Source Classification
Zingiberaceae
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COX
NF-κB
TNF Receptor
Interleukin Related
Apoptosis
VEGFR
Bacterial
Dengue Virus
Caspase
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4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC50 = 1.12 μM) and COX-2 (IC50 = 0.83 μM)), NF-κB (IC50 = 88.7 μM) and cytokine production (TNF-α (IC50 = 96.84 μg/mL) and IL-1β (IC50 = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats .
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- HY-N4219
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- HY-N11960
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- HY-N8290R
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- HY-N0398R
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- HY-N16538
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- HY-N8487R
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Flavonoids
Flavones
Leguminosae
Zornia brasiliensis
Plants
Source Classification
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Reference Standards
Cytochrome P450
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7-Methoxyflavone (Standard) is the analytical standard of 7-Methoxyflavone (HY-N8487). This product is intended for research and analytical applications. 7-Methoxyflavone is a flavonoid compound that can be isolated from Zornia brasiliensis. 7-Methoxyflavone can bind to human serum albumin and is an aromatase inhibitor. 7-Methoxyflavone has peripheral analgesic and certain antitumor activities. 7-Methoxyflavone is effective against chemical pain but has no significant effect on thermal pain .
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- HY-N18124
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Structural Classification
Melia azedarach Linn.
Ketones, Aldehydes, Acids
Plants
Meliaceae
Source Classification
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Others
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1-O-Tigloyl-1-O-debenzoylohchinal is an orally active limonoid-type triterpenoid anti-inflammatory and peripheral analgesic agent isolated from the fruits of Melia toosendan. 1-O-Tigloyl-1-O-debenzoylohchinal significantly inhibits acetic acid (HY-Y0319)-induced increase in vascular permeability, λ-Carrageenan (HY-N9470)-induced paw edema, and acetic acid-induced writhing response in mice. 1-O-Tigloyl-1-O-debenzoylohchinal shows no significant analgesic effect in the hot-plate test, and acts mainly on the peripheral rather than the central nervous system. 1-O-Tigloyl-1-O-debenzoylohchinal can be widely used in the research of acute or chronic inflammation, stomachache and other related diseases .
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Product Name |
Chemical Structure |
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- HY-B0527AS
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Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
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- HY-108449S
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Acoltremon-d3 (WS-12-d3) is the deuterium labeled Acoltremon (HY-108449). Acoltremon 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-109054AS
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O-Desmethyltramadol-d6 hydrochloride is a deuterated labeled O-Desmethyltramadol hydrochloride. O-Desmethyltramadol hydrochloride is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol hydrochloride mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR) .
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- HY-132428S
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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 .
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- HY-W050088S
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Isoxepac-d6 (HP 549-d6) is the deuterium labeled Isoxepac (HY-W050088). Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
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- HY-B0363S
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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 .
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- HY-B0363S1
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Nimesulide- 13C6 (R805- 13C6) is 13C 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.
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- HY-W777360
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Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-W700834
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Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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Product Name |
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Classification |
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- HY-159562
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Azide
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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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Azide
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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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