Search Result
Results for "
transient receptor potential channels
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-11062
-
Icilin
1 Publications Verification
AG-3-5
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response .
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-
-
- HY-B0545
-
-
-
- HY-101547
-
|
TRP Channel
|
Cancer
|
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
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-
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- HY-B0545S
-
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
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Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
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-
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- HY-19960
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BCTC
4 Publications Verification
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TRP Channel
Insulin Receptor
CGRP Receptor
|
Neurological Disease
Metabolic Disease
Cancer
|
BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects .
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-
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- HY-101323
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NE-19550; N-Vanillyloleamide
|
TRP Channel
|
Neurological Disease
|
Olvanil (NE-19550) is an analgesic and an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC50 of 0.7 nM .
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-
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- HY-B0545R
-
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
Cancer
|
Probenecid (Standard) is the analytical standard of Probenecid. This product is intended for research and analytical applications. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
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-
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- HY-108465
-
|
TRP Channel
|
Others
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Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
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-
-
- HY-N3230
-
Murraxocin
|
TRP Channel
|
Inflammation/Immunology
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Murpanicin (murraxocin) is a coumarin that is a thermosensitive transient receptor potential vanilloid 2 (TRPV2) channel inhibitor. Murpanicin has significant anti-inflammatory and insecticidal effects.
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-
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- HY-137704
-
|
TRP Channel
|
Others
|
2′-Deoxy-ADPR is an agonist for transient receptor potential melastatin 2 channel (TRPM2 channel). 2′-Deoxy-ADPR may acts as the signaling molecule in Jurkat T-lymphocytes .
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-
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- HY-W404916
-
|
TRP Channel
Bacterial
HIV
|
Infection
|
Probenecid sodium is the sodium salt of Probenecid. Probenecid is an effective selective transient receptor potential vanilloid 2 (TRPV2) agonist. Probenecid also inhibits the pannexin 1 channel .
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- HY-108461
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-
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- HY-117804
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8-Bromo-Cyclic ADP-Ribose
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TRP Channel
|
Neurological Disease
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8-Br-cADPR is a potent cADPR antagonist. 8-Br-cADPR reduces renal damage and the expression of caspase-3 and TRPM2 .
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- HY-121539
-
|
TRP Channel
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Neurological Disease
|
Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines .
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-
-
- HY-111036
-
|
TRP Channel
|
Others
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AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm) .
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- HY-19608
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-
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- HY-113654
-
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TRP Channel
|
Others
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AMG 7905 is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 potentiates TRPV1 channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin .
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- HY-75161
-
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TRP Channel
Endogenous Metabolite
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Cancer
|
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i . Antitumor activity .
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- HY-121841
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O-1821; CBD-C1
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TRP Channel
|
Inflammation/Immunology
Cancer
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Cannabidiorcol (CBDO, CBD-C1, O-1821) is related to cannabidiol, with the pentyl side chain shortened to a methyl group. Cannabidiorcol has low affinity for cannabinoid receptors (CBs) and is an agonist of the transient receptor potential channel (TRP channel), through which it produces antiinflammatory effects, but can also promote tumorigenesis at high concentrations .
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- HY-138668
-
|
TRP Channel
|
Cancer
|
JW-65 (compound 20) is a TRPC3 inhibitor. JW-65 can be used in neurological and cardiovascular disease related research .
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-
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- HY-132813
-
|
TRP Channel
|
Neurological Disease
|
Evifacotrep, a short transient receptor potential channel 5 and 4 (TRPC5/TRPC4) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases. Evifacotrep targets to TRPC5/TRPC4 with IC50s ≤50 nM .
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- HY-19765
-
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TRP Channel
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Cardiovascular Disease
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GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research .
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-
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- HY-12949
-
|
TRP Channel
|
Neurological Disease
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
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- HY-12949A
-
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TRP Channel
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Neurological Disease
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ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
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- HY-110199
-
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TRP Channel
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Neurological Disease
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models .
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- HY-148129
-
|
TRP Channel
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Cardiovascular Disease
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TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system .
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- HY-75161R
-
|
TRP Channel
Endogenous Metabolite
|
Cancer
|
(-)-Menthol (Standard) is the analytical standard of (-)-Menthol. This product is intended for research and analytical applications. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i . Antitumor activity .
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- HY-145150
-
|
TRP Channel
|
Metabolic Disease
|
TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD) .
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-
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- HY-110181
-
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TRP Channel
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Metabolic Disease
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M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb) .
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-
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- HY-19976
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RN-1747
2 Publications Verification
|
TRP Channel
|
Cardiovascular Disease
|
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM .
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-
-
- HY-103337
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Arachidonyl serotonin; AA-5-HT
|
FAAH
TRP Channel
|
Neurological Disease
|
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC50=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents .
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- HY-N0361
-
-
-
- HY-120964
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Stearoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling.
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- HY-120963
-
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Endogenous Metabolite
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Metabolic Disease
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Several different arachidonoyl amino acids, including N-arachidonoyl dopamine and N-arachidonoyl serine, have been isolated and characterized from bovine brain.1 During mass spectral lipidomics analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, were discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Oleoyl taurine is an amino-acyl endocannabinoid isolated from rat brain that may activate TRPV1 and TRPV4.
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- HY-110091
-
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TRP Channel
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Neurological Disease
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TRPV1 antagonist 9 (compound 13c) is an orally active transient receptor potential vanilloid 1 (TRPV1) channel antagonist. TRPV1 antagonist 9 blocks Ca 2+ uptake by CHO cells expressing TRPV1 receptors with IC50 values are 0.6 and 0.8 nM for Capsaicin (HY-10448) and acid-induced Ca 2+ uptake, respectively. TRPV1 antagonist 9 blocks Capsaicin (HY-10448)-induced flinch response and causes hyperthermia in rats .
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- HY-N0361R
-
|
TRP Channel
Reactive Oxygen Species
Apoptosis
Caspase
Bcl-2 Family
Akt
PI3K
|
Cardiovascular Disease
Neurological Disease
|
Dihydrocapsaicin (Standard) is the analytical standard of Dihydrocapsaicin. This product is intended for research and analytical applications. Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
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-
- HY-173024
-
|
TRP Channel
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Neurological Disease
|
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
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- HY-N0361S
-
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Isotope-Labeled Compounds
Apoptosis
Bcl-2 Family
Reactive Oxygen Species
TRP Channel
Caspase
PI3K
Akt
|
Others
|
Dihydrocapsaicin-d3 is the deuterium labeled Dihydrocapsaicin (HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
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- HY-121465
-
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Endogenous Metabolite
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Metabolic Disease
|
Stearoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of fatty acid amide hydrolase (FAAH) and the transient receptor potential vanilloid-type 1 (TRPV1) channel, reducing both acute and chronic peripheral pain. The effects of replacing the arachidonoyl portion with the saturated 18-carbon stearoyl moiety have not been studied. However, replacement of arachidonate with saturated 11- or 12-carbon fatty acids produces compounds that potently inhibit capsaicin-induced TRPV1 channel activation (IC50=0.76 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC50 > 50 μM).
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- HY-B1173
-
D-(+)-Camphor; (1R)-(+)-Camphor
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Bacterial
|
Neurological Disease
Inflammation/Immunology
Cancer
|
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
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-
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- HY-B1173R
-
D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
|
Bacterial
|
Neurological Disease
Inflammation/Immunology
Cancer
|
(+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
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- HY-139192
-
NMDAR/TRPM4-IN-2
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iGluR
TRP Channel
ERK
|
Neurological Disease
|
Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
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-
-
- HY-139192A
-
NMDAR/TRPM4-IN-2 free base
|
iGluR
TRP Channel
ERK
|
Neurological Disease
|
Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
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-
-
- HY-126720
-
|
Endogenous Metabolite
|
Metabolic Disease
|
N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
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-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-75161
-
-
-
- HY-75161R
-
-
-
- HY-N0361
-
-
-
- HY-B1173
-
D-(+)-Camphor; (1R)-(+)-Camphor
|
Structural Classification
Other Monoterpenes
Classification of Application Fields
Terpenoids
Source classification
Other Diseases
Plants
Lauraceae
Cinnamomum camphora
Disease Research Fields
|
Bacterial
|
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
-
- HY-N3230
-
-
-
- HY-N0361R
-
-
-
- HY-B1173R
-
D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
|
Structural Classification
Other Monoterpenes
Terpenoids
Source classification
Plants
Lauraceae
Cinnamomum camphora
|
Bacterial
|
(+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0545S
-
|
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
|
-
-
- HY-N0361S
-
|
Dihydrocapsaicin-d3 is the deuterium labeled Dihydrocapsaicin (HY-N0361) . Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat .
|
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Cat. No. |
Product Name |
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Classification |
-
- HY-75161
-
|
|
Flavoring Agents
|
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i . Antitumor activity .
|
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