Search Result
Results for "
Nociceptive
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-70050C
-
GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
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-
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- HY-106224
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Hypocretin-1 (human, rat, mouse)
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Orexin Receptor (OX Receptor)
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Neurological Disease
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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-
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- HY-155616
-
|
Sigma Receptor
Histamine Receptor
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Neurological Disease
|
KSK94 is a high-affinity histamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .
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-
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- HY-155615
-
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
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-
-
- HY-108960
-
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P2X Receptor
|
Inflammation/Immunology
|
PPADS is a P2 receptor antagonist, with IC50s of 68 nM (P2X1) and 214 nM (P2X3). PPADS acts as an ATP (nucleotide) mimetic and competes with ATP for its binding site on P2 receptors. PPADS is also a reversible competitive antagonist of the NAADP receptor. PPADS reverses nociceptive hypersensitivity and reduces the increased NO/NOS system and IL-1β in both peripheral and central steps of nervous system .
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-
-
- HY-142699
-
|
Somatostatin Receptor
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Inflammation/Immunology
|
SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107) .
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-
-
- HY-155614
-
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
|
-
-
- HY-70050A
-
GR 68755; GR 68755X
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
-
- HY-70050
-
GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
-
- HY-70050B
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GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
-
- HY-106224A
-
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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-
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- HY-119820
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SR57746A free base
|
5-HT Receptor
|
Neurological Disease
|
Xaliproden free base is an orally active and selective 5-HT1A receptor agonist. Xaliproden free base shows analgesic effect against acute tonic nociceptive pain and has neuroprotective effects. Xaliproden free base has an acute inhibitory effect on paclitaxel (HY-B0015)-induced mechanical allodynia by inhibiting the excessive response of primary afferent neurons .
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-
-
- HY-N9615
-
-
-
- HY-135013
-
|
TRP Channel
|
Neurological Disease
|
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism .
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-
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- HY-B2082
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-
-
- HY-108479
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SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
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-
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- HY-137988
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-
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- HY-B2114
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Escin
2 Publications Verification
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Escin, a natural compound of triterpenoid saponins that can be isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent .
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-
-
- HY-P3499
-
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
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-
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- HY-100197
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N-Docosahexaenoyl ethanolamine (DHEA); Docosahexaenoyl ethanolamide
|
Cannabinoid Receptor
|
Neurological Disease
|
Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .
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-
-
- HY-Y0892
-
-
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- HY-N0746
-
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Others
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Cancer
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Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides.?Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems . Oxysophocarpine inhibits the?growth?and?metastasis?of ?oral?squamous?cell?carcinoma?(OSCC) .
|
-
-
- HY-100326
-
-
-
- HY-104006
-
|
Opioid Receptor
|
Neurological Disease
|
CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
|
-
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- HY-151392
-
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Others
|
Neurological Disease
Inflammation/Immunology
|
LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains .
|
-
-
- HY-117061
-
|
Prostaglandin Receptor
|
Endocrinology
|
Prostaglandin F2α alcohol methyl ether is an alcohol methyl ether G protein-coupled receptor. Prostaglandin F2α is also a luteinizing hormone in sheep and may be a nociceptive mediator in the spinal cord .
|
-
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- HY-120308
-
SR140603
|
Neurokinin Receptor
|
Neurological Disease
|
(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
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-
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- HY-130660
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Prostamide F2α
|
Prostaglandin Receptor
|
Endocrinology
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Prostaglandin F2α ethanolamide (Prostamide F2α) is an ethanolamide-like G protein-coupled receptor. Prostaglandin F2α is also a luteinizing hormone in sheep and may be a nociceptive mediator in the spinal cord .
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-
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- HY-18978
-
|
Adenosine Receptor
|
Inflammation/Immunology
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GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions .
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-
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- HY-N2165
-
-
-
- HY-136207
-
|
nAChR
|
Neurological Disease
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
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-
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- HY-P1213A
-
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Melanocortin Receptor
|
Neurological Disease
|
JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
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-
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- HY-P1213
-
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Melanocortin Receptor
|
Neurological Disease
|
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
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- HY-N8487
-
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Others
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Neurological Disease
Inflammation/Immunology
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7-Methoxyflavone is a compound isolated from Zornia brasiliensis. 7-Methoxyflavone has peripheral antinociceptive activity. 7-Methoxyflavone inhibits paw-licking time in the neurogenic phase of the formalin pain response (65.6%) and did not decrease the nociceptive response in the inflammatory phase .
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- HY-117506B
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SBFI-26
1 Publications Verification
|
FABP
|
Neurological Disease
Inflammation/Immunology
|
SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects .
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-
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- HY-114810
-
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Prostaglandin Receptor
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Endocrinology
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Prostaglandin F2α serinol amide is a serinolamide G protein-coupled receptor that increases calcium levels in human non-small cell lung cancer cells. Prostaglandin F2α is also a luteinizing hormone in sheep and may be a nociceptive mediator in the spinal cord .
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- HY-N0746R
-
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Others
|
Cancer
|
Oxysophocarpine (Standard) is the analytical standard of Oxysophocarpine. This product is intended for research and analytical applications. Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems . Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) .
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-
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- HY-N6663
-
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COX
|
Inflammation/Immunology
|
3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
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- HY-159171
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-
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- HY-12741
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LDN-212320
Maximum Cited Publications
6 Publications Verification
LDN-0212320; OSU-0212320
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EAAT
|
Neurological Disease
|
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC [1]
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-
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- HY-N5025
-
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P2X Receptor
Apoptosis
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Inflammation/Immunology
Cancer
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses . Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed .
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-
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- HY-130605
-
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P2X Receptor
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Neurological Disease
|
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects .
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-
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- HY-10635
-
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TRP Channel
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Inflammation/Immunology
Cancer
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ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .
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- HY-N1500
-
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TRP Channel
Endogenous Metabolite
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Inflammation/Immunology
|
Pulegone, the major chemical constituent of Nepeta catariaessential oil which is an aromatic herb, is one of avian repellents . The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations .
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- HY-Y0892R
-
|
Apoptosis
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
4-Hydroxybenzyl alcohol (Standard) is the analytical standard of 4-Hydroxybenzyl alcohol. This product is intended for research and analytical applications. 4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth [4].
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-
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- HY-N6967
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(-)-α-Bisabolol
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Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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-
-
- HY-125527A
-
17(R)-RvD1; AT-RvD1
|
TRP Channel
|
Inflammation/Immunology
|
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
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-
-
- HY-W014421
-
|
TRP Channel
|
Neurological Disease
|
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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-
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- HY-P1399
-
Myr-Pep2m
|
PKC
|
Neurological Disease
|
Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC) .
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-
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- HY-108425A
-
|
Sodium Channel
|
Neurological Disease
|
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
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-
- HY-P1399A
-
Myr-Pep2m TFA
|
PKC
|
Neurological Disease
|
Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC) .
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-
- HY-N1500R
-
|
TRP Channel
Endogenous Metabolite
|
Inflammation/Immunology
|
Pulegone (Standard) is the analytical standard of Pulegone. This product is intended for research and analytical applications. Pulegone, the major chemical constituent of Nepeta catariaessential oil which is an aromatic herb, is one of avian repellents . The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations .
|
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- HY-N6663R
-
|
COX
|
Inflammation/Immunology
|
3-Carene (Standard) is the analytical standard of 3-Carene. This product is intended for research and analytical applications. 3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
|
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- HY-13509
-
|
RGS Protein
|
Inflammation/Immunology
|
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
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- HY-142700
-
|
Somatostatin Receptor
|
Neurological Disease
|
SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14) .
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- HY-142701
-
|
Somatostatin Receptor
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Neurological Disease
|
SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14) .
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- HY-N5142S1
-
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Bacterial
Isotope-Labeled Compounds
|
Infection
|
α-Terpineol-d6 is deuterated labeled Pulegone (HY-N1500). Pulegone, the major chemical constituent of Nepeta catariaessential oil which is an aromatic herb, is one of avian repellents . The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations .
|
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- HY-N6967R
-
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Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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- HY-P1626
-
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Opioid Receptor
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Neurological Disease
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Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
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- HY-B0380B
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GIC-1001
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Others
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Others
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Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
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-
- HY-108425B
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(Rac)-AMG8380
|
Sodium Channel
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Neurological Disease
|
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
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- HY-145169
-
|
Sodium Channel
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Neurological Disease
|
AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects .
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- HY-P10358
-
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Calcium Channel
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Neurological Disease
|
TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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- HY-70050CR
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GR 68755C (Standard); GR 68755 Hydrochloride (Standard); GR 68755X Hydrochloride (Standard)
|
5-HT Receptor
|
Neurological Disease
|
Alosetron (Hydrochloride) (Standard) is the analytical standard of Alosetron (Hydrochloride). This product is intended for research and analytical applications. Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
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-
- HY-117694
-
|
CGRP Receptor
|
Neurological Disease
Inflammation/Immunology
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MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine .
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- HY-108425
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Sodium Channel
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Neurological Disease
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AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
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- HY-N4226
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AP-1
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Inflammation/Immunology
Cancer
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1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function .
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- HY-149335
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Sigma Receptor
Histamine Receptor
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Neurological Disease
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Sigma-1 receptor antagonist 5 (compound 12),a 4-pyridylpiperidine derivative with analgesic activity,is an antagonist of sigma receptor (Ki=4.5 nM (σ1R),10 nM (σ2R)) and histamine H3 (hH3R,Ki=7.7 nM,IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .
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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
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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-15026
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Endogenous Metabolite
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Inflammation/Immunology
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ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-106224
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Hypocretin-1 (human, rat, mouse)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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- HY-106224A
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Hypocretin-1 (human, rat, mouse) (TFA)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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- HY-P3499
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Guanylate Cyclase
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Inflammation/Immunology
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Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
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- HY-P1213
-
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Melanocortin Receptor
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Neurological Disease
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JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
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-
- HY-P1399A
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Myr-Pep2m TFA
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PKC
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Neurological Disease
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Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC) .
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- HY-P1626
-
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Opioid Receptor
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Neurological Disease
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Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
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- HY-P1213A
-
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Melanocortin Receptor
|
Neurological Disease
|
JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect .
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- HY-P1399
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Myr-Pep2m
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PKC
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Neurological Disease
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Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC) .
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-
- HY-P10358
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|
Calcium Channel
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Neurological Disease
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TAT-CBD3A6K, is a modified TAT-CBD3 peptide. TAT-CBD3A6K reduces T- and R-type voltage-dependent calcium currents in dorsal root ganglion (DRG) neurons. TAT-CBD3A6K shows anti-nociceptive effects in a model of AIDS-induced peripheral neuropathy by preventing CRMP-2-mediated enhancement of T- and R-type calcium channel function .
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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
-
|
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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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-135013
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-
-
- HY-B2114
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-
-
- HY-Y0892
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-
-
- HY-N0746
-
-
-
- HY-N2165
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-
-
- HY-N8487
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-
-
- HY-N6663
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-
-
- HY-N9615
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-
-
- HY-137988
-
-
-
- HY-N0746R
-
-
-
- HY-N5025
-
-
-
- HY-N1500
-
-
-
- HY-Y0892R
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-
-
- HY-N6967
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(-)-α-Bisabolol
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Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Apoptosis
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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-
-
- HY-N1500R
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-
-
- HY-N6663R
-
|
Structural Classification
Other Monoterpenes
other families
Terpenoids
Source classification
Plants
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COX
|
3-Carene (Standard) is the analytical standard of 3-Carene. This product is intended for research and analytical applications. 3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
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-
-
- HY-N6967R
-
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
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Apoptosis
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Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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-
-
- HY-N4226
-
|
Structural Classification
Microorganisms
other families
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Plants
Disease Research Fields
Cancer
|
AP-1
|
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N5142S1
-
|
α-Terpineol-d6 is deuterated labeled Pulegone (HY-N1500). Pulegone, the major chemical constituent of Nepeta catariaessential oil which is an aromatic herb, is one of avian repellents . The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations .
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Cat. No. |
Product Name |
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Classification |
-
- HY-151391
-
|
|
Alkynes
|
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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