Search Result
Isoforms Recommended: |
TRPV
|
Results for "
TRPV1)
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-144372
-
|
TRP Channel
|
Neurological Disease
|
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant [1].
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-
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- HY-148751
-
|
TRP Channel
|
Cancer
|
TRPV1 activator-1 (compound 8), a capsaicin analog, has an altered neck structure. TRPV1 activator-1 interacts specifically with T551 residue [1].
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-
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- HY-111218
-
-
-
- HY-161420
-
|
TRP Channel
|
Neurological Disease
|
TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 antagonist that effectively blocks capsaicin activation (IC50=2.31 nM). TRPV1 antagonist 7 can be used in analgesic research [1].
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-
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- HY-110091
-
|
TRP Channel
|
Neurological Disease
|
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 [1].
|
-
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- HY-148752
-
|
TRP Channel
|
Metabolic Disease
|
TRPV1 activator-2 (compound 9), a capsaicin head analog, makes specific interactions with channel residues at the lipid-water [1].
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-
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- HY-161273
-
|
TRP Channel
|
Neurological Disease
|
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration [1].
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-
-
- HY-RS15121
-
|
Small Interfering RNA (siRNA)
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Others
|
TRPV1 Human Pre-designed siRNA Set A contains three designed siRNAs for TRPV1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
TRPV1 Human Pre-designed siRNA Set A
TRPV1 Human Pre-designed siRNA Set A
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- HY-P10465
-
|
TRP Channel
|
Inflammation/Immunology
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain [1].
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-
-
- HY-162856
-
-
-
- HY-162908
-
-
-
- HY-157766
-
|
FAAH
TRP Channel
|
Inflammation/Immunology
|
FAAH/TRPV1 blocker-1 (compound 2R) is a dual FAAH/TRPV1 blocker, with IC50 of 0.12 and 94.9 μM, respectively. FAAH/TRPV1 blocker-1 plays an important role in analgesic and anti-inflammatory research [1].
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-
-
- HY-P1175
-
|
TRP Channel
|
Neurological Disease
|
L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic [1] .
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-
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- HY-P1175A
-
|
TRP Channel
|
Neurological Disease
|
L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic [1] .
|
-
-
- HY-109841
-
-
-
- HY-12428
-
-
-
- HY-128479
-
-
-
- HY-101736
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AMG9810
4 Publications Verification
|
TRP Channel
|
Neurological Disease
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
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-
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- HY-121122
-
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Others
|
Others
|
A778317 is a TRPV1 antagonists. A778317 can block changes in intracellular calcium levels mediated by TRPV1 receptors, with a pIC50 value of 8.31. A-778317 can also block the activation of natural rat TRPV1 receptors in dorsal root ganglion neurons by capsaicin and acid [1].
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- HY-111038
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Coniferyl (E)-8-methyl-6-nonenoate
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
Capsiconiate (Coniferyl (E)-8-methyl-6-nonenoate) is a TRPV1 agonist (EC50= 3.2 μM). Capsiconiate can be used to study TRPV1-mediated diseases such as pain, inflammation, and epilepsy(EC50= 3.2 μM) [1].
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- HY-110209
-
|
TRP Channel
|
Others
|
AC4 is a trans antagonist upon voltageactivation of TRPV1 and as cis antagonist of TRPV1 currents upon stimulation with Capsaicin (HY-10448). AC4 demonstrates that a photoswitchable antagonist and an agonist can be used in concert [1].
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- HY-117683
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TRP Channel
|
Neurological Disease
|
BCTP is a TRPV1 antagonist. BCTP activated at low pH showed functional antagonist activity against human TRPV1 in CHO cells (IC50=18 nM). BCTP can be used in the study of chronic pain [1].
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- HY-100668
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-
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- HY-108458
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-
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- HY-108448
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OLDA
|
TRP Channel
|
Cardiovascular Disease
|
N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1 [1] .
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- HY-113654
-
|
TRP Channel
|
Others
|
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 [1] .
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- HY-N2333
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(+)-Resiniferatoxin
|
TRP Channel
|
Cardiovascular Disease
Cancer
|
Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period [1] .
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- HY-15640
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TRP Channel
Apoptosis
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Cancer
|
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
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- HY-N0172
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-
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- HY-W554764
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-
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- HY-10634
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-
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- HY-W747573
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18:3 NAE; α-Linolenoyl ethanolamide
|
TRP Channel
|
Neurological Disease
|
N-Linolenoylethanolamine (18:3 NAE) is an endocannabinoid. N-Linolenoylethanolamine is a vanillin receptor (TRPV1) agonist [1].
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- HY-123428
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-
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- HY-12777
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-
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- HY-B1583
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Zucapsaicin; Civamide; cis-Capsaicin
|
TRP Channel
HSV
|
Neurological Disease
|
(Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.
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- HY-P10464
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TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
TAT-AKAP79 326-336 is a cytoosmotic peptide. TAT-AKAP79 326-336 mimics a specific region on the AKAP79 protein that binds to TRPV1 ion channels (amino acid sequence 326-336). TAT-AKAP79 326-336 inhibits the sensitization of TRPV1 and reduce the overresponse of TRPV1 channels to stimuli caused by the activation of cellular kinases such as protein kinase A (PKA) and protein kinase C (PKC) by inflammatory mediators. TAT-AKAP79 326-336 can be used to study the mechanism of pain transduction and inflammatory hyperalgesia [1].
|
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- HY-108460
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|
TRP Channel
|
Neurological Disease
|
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration [1].
|
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- HY-12245
-
|
TRP Channel
|
Inflammation/Immunology
|
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation [1] .
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- HY-124073
-
|
TRP Channel
|
Metabolic Disease
|
Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease [1].
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- HY-114630
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-
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- HY-10635A
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-
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- HY-P10654
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-
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- HY-110292
-
|
TRP Channel
|
Inflammation/Immunology
|
A-425619, a potent and selective TRPV1 receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain [1].
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- HY-117922
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- HY-100129
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TRP Channel
|
Neurological Disease
|
JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine [1] .
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- HY-101323
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NE-19550; N-Vanillyloleamide
|
TRP Channel
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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 [1].
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- HY-118785
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-
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- HY-132596A
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SYL1001 sodium
|
TRP Channel
|
Neurological Disease
|
Tivanisiran sodium is a siRNA used for the study of dry eye disease. Tivanisiran sodium was designed to silence transient receptor potential vanilloid 1 (TRPV1) mRNA [1].
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- HY-158110
-
|
TRP Channel
|
Inflammation/Immunology
|
Phenylcapsaicin is an analogue of Capsaicin (HY-10448). Phenylcapsaicin is a TRPV1 receptor activator. Phenylcapsaicin enhances fat oxidation during aerobic exercise [1] .
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- HY-10633
-
|
TRP Channel
|
Neurological Disease
|
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
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- HY-17568
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Pelargonic acid vanillylamide; Nonanoic acid vanillylamide; Pseudocapsaicin
|
TRP Channel
|
Neurological Disease
|
Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
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- HY-103368
-
|
Chloride Channel
|
Neurological Disease
|
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity [1].
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- HY-N8377
-
|
TRP Channel
|
Inflammation/Immunology
|
Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1 [1].
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- HY-132596
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- HY-W517163
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-
- HY-114017
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-
- HY-108576
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DuP 996 dihydrochloride
|
TRP Channel
|
Neurological Disease
|
Linopirdine dihydrochloride is a agonist of capsaicin receptor TRPV1. Linopirdine increases the intracellular calcium concentration in HEK293 cells. Linopirdine dihydrochloride exerts an excitatory action on mammalian nociceptors [1].
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- HY-123374
-
|
TRP Channel
|
Neurological Disease
|
(Rac)-AMG 628 is the racemate of AMG 628, a potent TRPV1 antagonist with an IC50 of 3.7nM. AMG 628 can be used in chronic pain research [1].
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- HY-12195
-
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- HY-10448A
-
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- HY-137459
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CA-008
|
TRP Channel
|
Neurological Disease
|
Vocacapsaicin (CA-008), a proagent of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief [1].
|
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- HY-137459A
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CA-008 hydrochloride
|
TRP Channel
|
Neurological Disease
|
Vocacapsaicin (CA-008) hydrochloride, a proagent of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride can provide meaningful and long-lasting pain relief [1].
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- HY-110018
-
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- HY-120962
-
|
TRP Channel
|
Metabolic Disease
|
N-Arachidonoyl Taurine is an activator of the transient receptor potential vanilloid TRPV1 and TRPV4, with EC50s value of 28 μM and 21 μM, respectively [1].
|
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- HY-137988
-
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- HY-10448
-
-
- HY-101389
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- HY-124382
-
|
TRP Channel
|
Neurological Disease
|
AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research [1].
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- HY-124073R
-
|
TRP Channel
|
Metabolic Disease
|
Dihydrocapsiate (Standard) is the analytical standard of Dihydrocapsiate. This product is intended for research and analytical applications. Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease [1].
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- HY-B1583R
-
|
TRP Channel
HSV
|
Neurological Disease
|
(Z)-Capsaicin (Standard) is the analytical standard of (Z)-Capsaicin. This product is intended for research and analytical applications. (Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.
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- HY-108455
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PALDA
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Others
|
Neurological Disease
|
N-Palmitoyl dopamine (PALDA) is a endogenous, long-chain, linear fatty acid dopamide, which is inactive on TRPV1. N-Palmitoyl dopamine displays 'entourage' effects on endovanilloids N-arachidonoyl-dopamine (NADA) and anandamide [1].
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- HY-110145
-
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TRP Channel
|
Cancer
|
MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis [1] .
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- HY-16413
-
Caytine hydrochloride; JB-251 hydrochloride
|
TRP Channel
Adrenergic Receptor
|
Others
|
Protokylol hydrochloride (Caytine hydrochloride; JB-251 hydrochloride) is the hydrochloride salt form of Protokylol (HY-114630). Protokylol hydrochloride is an agonist for β2-adrenergic receptor and TRPV1. Protokylol hydrochloride exhibits activity as a bronchodilator [1].
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- HY-N7536
-
|
TRP Channel
|
Others
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana [1].
|
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- HY-19589
-
-
- HY-120476
-
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs [1].
|
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- HY-17568R
-
|
TRP Channel
|
Neurological Disease
|
Nonivamide (Standard) is the analytical standard of Nonivamide. This product is intended for research and analytical applications. Nonivamide is a <b<TRPV1 agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
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- HY-N0285
-
-
- HY-10448S1
-
-
- HY-N0447
-
-
- HY-111036
-
|
TRP Channel
|
Others
|
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) [1].
|
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- HY-N2941
-
|
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
Bisandrographolide C is an unusual dimer of ent-labdane diterpenoid isolated and identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels with Kd values of 289 and 341 μM respectively, and protects cardiomyocytes from hypoxia-reoxygenation injury [1].
|
-
- HY-120294
-
|
CGRP Receptor
TRP Channel
|
Neurological Disease
|
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research [1].
|
-
- HY-N6825
-
-
- HY-10448R
-
(E)-Capsaicin (Standard)
|
TRP Channel
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
Capsaicin (Standard) is the analytical standard of Capsaicin. This product is intended for research and analytical applications. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects [1] .
|
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- HY-10448S4
-
-
- HY-167868
-
|
TRP Channel
Apoptosis
|
Neurological Disease
Cancer
|
DWP-05195 is a TRPV1 antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells [1] .
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- HY-121465
-
|
Endogenous Metabolite
|
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-10448AR
-
-
- HY-W020468
-
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue [1] .
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- HY-P3467
-
-
- HY-16935
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JNJ-39439335
|
TRP Channel
|
Neurological Disease
|
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain [1].
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- HY-121636
-
RvD2
|
TRP Channel
|
Infection
Neurological Disease
Inflammation/Immunology
|
Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons [1] .
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- HY-135882
-
-
- HY-147707
-
|
Cannabinoid Receptor
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Others
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
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- HY-N0285R
-
|
Cholinesterase (ChE)
TRP Channel
|
Neurological Disease
|
Imperatorin (Standard) is the analytical standard of Imperatorin. This product is intended for research and analytical applications. Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
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- HY-18662
-
|
TRP Channel
|
Neurological Disease
Cancer
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels [1] .
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- HY-136363
-
|
TRP Channel
|
Neurological Disease
|
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity [1].
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- HY-10635
-
|
TRP Channel
|
Inflammation/Immunology
Cancer
|
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 [1] .
|
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- HY-133166
-
|
TRP Channel
|
Neurological Disease
|
A-889425 is an oral active selective TRPV1 receptor antagonist with the with an IC50 of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws [1] .
|
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- HY-19960
-
BCTC
3 Publications Verification
|
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 [1] .
|
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- HY-135881
-
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM) [1].
|
-
- HY-103337
-
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 [1].
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- HY-N0447R
-
|
TRP Channel
Bacterial
|
Infection
Inflammation/Immunology
Cancer
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8-Gingerol (Standard) is the analytical standard of 8-Gingerol. This product is intended for research and analytical applications. 8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 μM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro [1] .
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- HY-120174
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Others
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Others
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SU200 is a TRPV1 agonist with the activity of regulating intracellular calcium ion concentration. SU200 can induce different calcium ion response modes, showing significant reaction potential and maximum reaction effect. There is obvious response delay and variability in the effects of SU200 in different cells. The use of SU200 may provide pharmacological development opportunities [1].
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- HY-160900
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TRP Channel
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Others
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RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively [1].
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- HY-N8264
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TRP Channel
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Neurological Disease
Inflammation/Immunology
Cancer
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Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities [1] .
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- HY-131986
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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LASSBio-1135 (Compound 3a) is an orally active TRPV1 antagonist. LASSBio-1135 is an anti-inflammatory and analgesic compound. LASSBio-1135 inhibits moderately the human PGHS-2 enzyme activity (IC50 = 18.5 μM). LASSBio-1135 reverts the Capsaicin (HY-10448)-induced thermal hyperalgesia and reduces the carrageenan-induced rat paw edem [1].
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- HY-101507
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Pico145; HC-608
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TRP Channel
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Cancer
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Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 [1].
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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 [1].
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- HY-N0361
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- HY-W708469
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Endogenous Metabolite
TRP Channel
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Inflammation/Immunology
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Resolvin D2 methyl ester is an ester derivative of the DHA (HY-B2167) metabolite Resolvin D2 (HY-121636) with anti-inflammatory and anti-infective activities. Resolvin D2 is a leukocyte modulator and a potent inhibitor of neuronal TRPV1 (IC50=0.1 nM) and TRPA1 (IC50=2 nM). Resolvin D2 can be used in sepsis research [1] .
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- HY-121636S
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RvD2-d5
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TRP Channel
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Infection
Neurological Disease
Inflammation/Immunology
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Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
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- HY-N6962
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TRP Channel
COX
Bacterial
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Infection
Neurological Disease
Metabolic Disease
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α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC50 values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice [1] .
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- HY-107436
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LE135
1 Publications Verification
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RAR/RXR
TRP Channel
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Neurological Disease
Cancer
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LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5?μM and 20?μM, respectively [1] .
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- HY-157131
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TRP Channel
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Neurological Disease
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TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+ influx in macrophages, and inhibits macrophage phagocytosis [1].
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- HY-10863
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- HY-N0361S
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Isotope-Labeled Compounds
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Others
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Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) [1]. 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-N0361R
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TRP Channel
Reactive Oxygen Species
Apoptosis
Caspase
Bcl-2 Family
Akt
PI3K
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Cardiovascular Disease
Neurological Disease
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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 [1] .
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- HY-10863S
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AEA-d8
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Isotope-Labeled Compounds
Cannabinoid Receptor
PPAR
Endogenous Metabolite
Tau Protein
GPR55
Fungal
TRP Channel
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Infection
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Anandamide-d8 is a deuterated labeled Anandamide [1]. Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
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- HY-150030
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Cannabinoid Receptor
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Neurological Disease
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CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively [1].
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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-105285
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Neu-P11
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Melatonin Receptor
5-HT Receptor
P2X Receptor
TRP Channel
Sodium Channel
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Neurological Disease
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Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities [1] .
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- HY-P1441A
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Sodium Channel
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Neurological Disease
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Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
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- HY-101448
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WAY-171318
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MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions [1] .
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- HY-126720
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Endogenous Metabolite
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Metabolic Disease
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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 |
Target |
Research Area |
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- HY-P3467
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- HY-P1441A
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Sodium Channel
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Neurological Disease
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Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
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- HY-P10465
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TRP Channel
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Inflammation/Immunology
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TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain [1].
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- HY-P1175
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TRP Channel
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Neurological Disease
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L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic [1] .
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- HY-P1175A
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TRP Channel
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Neurological Disease
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L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic [1] .
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- HY-P10464
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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TAT-AKAP79 326-336 is a cytoosmotic peptide. TAT-AKAP79 326-336 mimics a specific region on the AKAP79 protein that binds to TRPV1 ion channels (amino acid sequence 326-336). TAT-AKAP79 326-336 inhibits the sensitization of TRPV1 and reduce the overresponse of TRPV1 channels to stimuli caused by the activation of cellular kinases such as protein kinase A (PKA) and protein kinase C (PKC) by inflammatory mediators. TAT-AKAP79 326-336 can be used to study the mechanism of pain transduction and inflammatory hyperalgesia [1].
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- HY-P10654
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-10863S
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Anandamide-d8 is a deuterated labeled Anandamide [1]. Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
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- HY-10448S1
-
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Capsaicin-d3 is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].
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- HY-10448S4
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Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects [1] .
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- HY-121636S
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Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
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- HY-N0361S
-
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Dihydrocapsaicin-d3is the deuterium labeledDihydrocapsaicin(HY-N0361) [1]. 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 |
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- HY-132596A
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SYL1001 sodium
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siRNAs
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Tivanisiran sodium is a siRNA used for the study of dry eye disease. Tivanisiran sodium was designed to silence transient receptor potential vanilloid 1 (TRPV1) mRNA [1].
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- HY-RS15121
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siRNAs
Pre-designed siRNA Sets
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TRPV1 Human Pre-designed siRNA Set A contains three designed siRNAs for TRPV1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-132596
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SYL1001
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siRNAs
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Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease. Tivanisiran was designed to silence transient receptor potential vanilloid 1 (TRPV1) [1].
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