Search Result
Results for "
Hyperalgesia
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-132268
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Calcium Channel
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Neurological Disease
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Cav 2.2 blocker 2 is a Cav2.2 calcium channel blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid .
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- HY-101911
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5-BDBD
2 Publications Verification
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P2X Receptor
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Neurological Disease
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5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG) .
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- HY-100617
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(S)-4-Carboxyphenylglycine
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mGluR
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Neurological Disease
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(S)-4CPG ((S)-4-Carboxyphenylglycine) is a potent mGluR2 agonist. (S)-4CPG reduces hyperalgesia and allodynia associated with sciatic nerve contraction injury in rats. (S)-4CPG can be used in research on neurological diseases .
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- HY-103177
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Adenosine Receptor
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Inflammation/Immunology
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PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice .
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- HY-11051
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Opioid Receptor
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Inflammation/Immunology
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JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
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- HY-P1319
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Opioid Receptor
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Inflammation/Immunology
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Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
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- HY-W014421
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TRP Channel
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Neurological Disease
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AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
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- HY-P1319A
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Opioid Receptor
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Inflammation/Immunology
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Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
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- HY-P3839
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Opioid Receptor
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Neurological Disease
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Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
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- HY-111615
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Somatostatin Receptor
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Neurological Disease
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J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
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- HY-111615A
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
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- HY-106841
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R-75231; R88021
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Others
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Inflammation/Immunology
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Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia .
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- HY-112738
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Phospholipase
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Inflammation/Immunology
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AX048 is an inhibitor for calcium-dependent phospholipase A2 cPLA2 with a XI(50) of 0.022 mole fraction and reveals an antihyperalgesic efficacy .
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- HY-P5873
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JZTX-X
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Potassium Channel
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Neurological Disease
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Jingzhaotoxin-X (JZTX-X) is a selective Kv4.2 and Kv4.3 potassium channels inhibitor. Jingzhaotoxin-X causes long-lasting mechanical hyperalgesia .
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- HY-102095
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mGluR
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Neurological Disease
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SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM .
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- HY-N2258
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Poncirin is isolated from Poncirus trifoliata with anti-inflammory activites. Poncirin significantly reduces mechanical hyperalgesia and allodynia in Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models .
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- HY-13283
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MF63
1 Publications Verification
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PGE synthase
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Inflammation/Immunology
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MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1 .
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- HY-103175
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Adenosine Receptor
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Neurological Disease
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PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia .
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- HY-B1496
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SKF 385 hemisulfate
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Monoamine Oxidase
Histone Demethylase
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Neurological Disease
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Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects .
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- HY-17447SA
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SKF 385-d5 hydrochloride
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Monoamine Oxidase
Histone Demethylase
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Neurological Disease
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Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
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- HY-146802
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout .
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- HY-147748
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COX
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Inflammation/Immunology
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COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase .
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- HY-131182
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Sodium Channel
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Neurological Disease
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DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects .
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- HY-P1726A
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Melanocortin Receptor
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MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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- HY-116099
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Prostaglandin Receptor
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Inflammation/Immunology
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ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research .
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- HY-151450
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- HY-13044
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- HY-18618
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Opioid Receptor
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Neurological Disease
Inflammation/Immunology
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SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
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- HY-18617
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Opioid Receptor
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Neurological Disease
Inflammation/Immunology
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rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
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- HY-110198
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Prostaglandin Receptor
PERK
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Inflammation/Immunology
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ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
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- HY-101249
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L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .
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- HY-108908
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- HY-12914
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain .
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- HY-110150
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UNC3230
5 Publications Verification
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Others
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Inflammation/Immunology
Cancer
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UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
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- HY-14485
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P2X Receptor
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Neurological Disease
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Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain .
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- HY-114072
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Opioid Receptor
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Neurological Disease
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J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors .
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- HY-146280
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GABA Receptor
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Neurological Disease
Metabolic Disease
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mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice .
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- HY-146281
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-111615A
-
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
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- HY-P3206
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Thymulin; Thymic factor
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Peptides
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Inflammation/Immunology
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Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide. Serum thymic factor induces hyperalgesia. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor has anti-diabetic, analgesic and anti-inflammatory effects .
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- HY-P1319
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Opioid Receptor
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Inflammation/Immunology
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Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
|
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- HY-P1319A
-
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Opioid Receptor
|
Inflammation/Immunology
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Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
|
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- HY-P3839
-
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Opioid Receptor
|
Neurological Disease
|
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
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- HY-P1020
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Peptides
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Neurological Disease
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Nocistatin (human) blocks nociceptin-induced allodynia and hyperalgesia, and attenuates pain evoked by prostaglandin E2 .
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- HY-P1020A
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Peptides
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Neurological Disease
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Nocistatin (human) TFA blocks nociceptin-induced allodynia and hyperalgesia, and attenuates pain evoked by prostaglandin E2 .
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- HY-P5873
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JZTX-X
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Potassium Channel
|
Neurological Disease
|
Jingzhaotoxin-X (JZTX-X) is a selective Kv4.2 and Kv4.3 potassium channels inhibitor. Jingzhaotoxin-X causes long-lasting mechanical hyperalgesia .
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- HY-P3856
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Peptides
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Neurological Disease
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Endokinin C is a peptide component of endokinin. Endokinin C works as a neurotransmitter or modulator in the pain system. Pretreatment with endokinin C prevents induction of scratching behavior and thermal hyperalgesia of endokinin A/B in mice .
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- HY-P1726A
-
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Melanocortin Receptor
|
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17447SA
-
|
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
|
-
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