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Results for "

TRPV1 antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Apoptosis (3) Bacterial (1) Calcium Channel (1) Cannabinoid Receptor (1) CGRP Receptor (2) COX (1) Cytochrome P450 (1) Endogenous Metabolite (1) ERK (1) FAAH (1) GLUT (1) HDAC (1) Histamine Receptor (1) Insulin Receptor (2) Interleukin Related (2) Isotope-Labeled Compounds (1) JNK (1) Melanocortin Receptor (3) Melatonin Receptor (2) NF-κB (1) Opioid Receptor (1) P2X Receptor (2) p38 MAPK (1) RAR/RXR (1) Reference Standards (10) Sodium Channel (2) TNF Receptor (2) TRP Channel (76) URAT1 (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (1) Endocrinology (2) Infection (3) Inflammation/Immunology (22) Metabolic Disease (7) Neurological Disease (50)

By Targets:

5-HT Receptor (2)

Apoptosis (3)

Bacterial (1)

Calcium Channel (1)

Cannabinoid Receptor (1)

CGRP Receptor (2)

COX (1)

Cytochrome P450 (1)

Endogenous Metabolite (1)

ERK (1)

FAAH (1)

GLUT (1)

HDAC (1)

Histamine Receptor (1)

Insulin Receptor (2)

Interleukin Related (2)

Isotope-Labeled Compounds (1)

JNK (1)

Melanocortin Receptor (3)

Melatonin Receptor (2)

NF-κB (1)

Opioid Receptor (1)

P2X Receptor (2)

p38 MAPK (1)

RAR/RXR (1)

Reference Standards (10)

Sodium Channel (2)

TNF Receptor (2)

TRP Channel (76)

URAT1 (1)

By Research Areas:

Cancer (11)

Cardiovascular Disease (1)

Endocrinology (2)

Infection (3)

Inflammation/Immunology (22)

Metabolic Disease (7)

Neurological Disease (50)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15640

Capsazepine Maximum Cited Publications 56 Publications Verification	TRP Channel Apoptosis	Cancer
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC₅₀ of 562 nM.

HY-101736

AMG9810 10+ Cited Publications	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.

HY-10634

AMG 517 5+ Cited Publications	TRP Channel	Neurological Disease
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC₅₀ of 0.5 nM.

HY-N0637

Eriodictyol 10+ Cited Publications Huazhongilexone	Melanocortin Receptor TRP Channel	Infection Inflammation/Immunology
Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active *TRPV1* receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the *TRPV1* receptor and activating the Nrf2 signaling pathway. Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases .

HY-12245

SB-366791 5+ Cited Publications	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 .

HY-10633

SB-705498 5+ Cited Publications	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.

HY-19960

BCTC 5 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 .

HY-12777

Asivatrep 1 Publications Verification PAC-14028	TRP Channel	Inflammation/Immunology
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

HY-N0637A

(±)-Eriodictyol (±)-Huazhongilexone; Dihydroluteolin	Melanocortin Receptor TRP Channel	Metabolic Disease
(±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active *TRPV1* receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the *TRPV1* receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases .

HY-18662

RQ-00203078 5+ Cited Publications	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 .

HY-144372

TRPV1 antagonist 3	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 .

HY-16935

Mavatrep JNJ-39439335	TRP Channel	Neurological Disease
Mavatrep (JNJ-39439335) is an orally active, selective and potent *TRPV1* antagonist with high affinity for hTRPV1 channels (K_i=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 .

HY-107436

LE135 4 Publications Verification	RAR/RXR TRP Channel	Neurological Disease Cancer
LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i 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 .

HY-N6962

α-Spinasterol	TRP Channel COX Bacterial	Infection Neurological Disease Metabolic Disease
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 .

HY-110292

A-425619	TRP Channel Calcium Channel	Inflammation/Immunology
A-425619 is an orally active and selective transient receptor potential type V1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca ²⁺ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury .

HY-N5084

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside	TRP Channel HDAC p38 MAPK JNK ERK NF-κB TNF Receptor Interleukin Related	Neurological Disease Inflammation/Immunology Cancer
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a *TRPV1* antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 ⁺ T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .

HY-100129

JNJ-17203212 1 Publications Verification	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 .

HY-12195

ABT-239 2 Publications Verification	Histamine Receptor TRP Channel	Neurological Disease Endocrinology
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

HY-113654

AMG 7905	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 .

HY-114017

Libvatrep SAF312; Vanilloid receptor antagonist 1	TRP Channel	Inflammation/Immunology
Vanilloid receptor antagonist 1 is a potent vanilloid receptor *TRPV1* antagonist extracted from patent US8349852B2, compound B8 .

HY-176063

TRPV1 antagonist 11	TRP Channel Opioid Receptor	Neurological Disease
TRPV1 antagonist 11 (compound 2ac) is a potent *TRPV1* antagonist with an IC₅₀ of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a K_i of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .

HY-161420

TRPV1 antagonist 7	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 .

HY-172774

TRPV1 antagonist 10	TRP Channel URAT1 GLUT Cytochrome P450 Interleukin Related TNF Receptor	Neurological Disease Inflammation/Immunology Endocrinology
TRPV1 antagonist 10 is an orally active and potent *TRPV1* antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain .

HY-160900

RN-1665 1 Publications Verification	TRP Channel	Others
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 .

HY-105285

Piromelatine 2 Publications Verification Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B 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 .

HY-109841

Oleoyl serotonin	TRP Channel	Neurological Disease
Oleoyl Serotonin (compound 1e) is a *TRPV1* antagonist with IC₅₀ value of 2.57 μM for human TRPV1 .

HY-108458

SB 452533	TRP Channel	Inflammation/Immunology
SB 452533 is a potent and selective *TRPV1* antagonist with the pK_b of 7.8 .

HY-N7536

Voacangine	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 .

HY-111218

TRPV1 antagonist 5	TRP Channel	Neurological Disease
TRPV1 antagonist 5 (compound 1) is a potent *TRPV1* antagonist .

HY-110091

TRPV1 antagonist 9	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 .

HY-103337

N-Arachidonoylserotonin 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 .

HY-161273

TRPV1 antagonist 6	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 .

HY-12428

A-1165442 2 Publications Verification	TRP Channel	Neurological Disease
A-1165442 is a potent, competitive and orally available *TRPV1* antagonist with an IC₅₀ of 9 nM for human TRPV1.

HY-P1175

L-R4W2	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 .

HY-10635

ABT-102	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 .

HY-100668

JYL 1421 SC 0030	TRP Channel	Neurological Disease
JYL 1421 is a TRPV1 receptor antagonist, with an IC₅₀ of 8 nM.

HY-105324

GRC-6211	TRP Channel	Inflammation/Immunology
GRC-6211 is an orally active and selective *TRPV1* antagonist. GRC-6211 exhibits anti-inflammation effect .

HY-105690

SAR-115740	TRP Channel	Neurological Disease Inflammation/Immunology
SAR-115740 is a *TRPV1* antagonist. SAR-115740 exhibits developmental toxicity in H9 cell experiments. SAR-115740 can be used for research on inflammatory conditions or neurological disorders .

HY-119121

JNJ-38893777	TRP Channel	Neurological Disease
JNJ-38893777 is an orally active and highly selective transient receptor potential vanilloid type 1 (TRPV1) channel antagonist. JNJ-38893777 inhibits neuronal hyperactivation and reduces inflammatory hyperalgesia. JNJ-38893777 is promising for research of migraine headaches, neuropathic and inflammatory pain .

HY-10635A

(S)-ABT-102	TRP Channel	Inflammation/Immunology Cancer
(S)-ABT-102 is a *TRPV1* Antagonist, with an IC₅₀ of 123 nM. (S)-ABT-102 has analgesic activity .

HY-12914

V116517	TRP Channel	Neurological Disease Inflammation/Immunology
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 .

HY-123374

(Rac)-AMG 628	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 .

HY-117372

DFL23448	TRP Channel	Metabolic Disease
DFL23448 is a selective transient receptor potential melastatin-8 (TRPM8) antagonist. DFL23448 shows IC₅₀ values of 10 and 21 nM in hTRPM8 human embryonic kidney 293 cells activated by Cooling Agent 10 or cold. DFL23448 has limited activity (IC₅₀ >10 μM) at transient receptor potential vanilloids TRPV1, TRPA1, or TRPV4 or at various G protein-coupled receptors. DFL23448 can modify bladder function and reduce bladder overactivity in awake rats .

HY-P10465

TRPV1-Tat	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 .

HY-110209

AC4	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 .

HY-117683

BCTP	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 .

HY-121122

A778317	TRP Channel	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 .

HY-113654A

AMG 7905 TFA	TRP Channel	Cardiovascular Disease
AMG 7905 TFA is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 TFA potentiates *TRPV1* channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin .

HY-W517163

MK-2295 NGD-8243	TRP Channel	Inflammation/Immunology
MK-2295 (NGD-8243) is a *TRPV1* antagonist. MK-2295 is an analgesic agent, and can be used for research of pain .

HY-15640R

Capsazepine (Standard)	TRP Channel Apoptosis Reference Standards	Cancer
Capsazepine (Standard) is the analytical standard of Capsazepine. This product is intended for research and analytical applications. Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.

Cat. No.	Product Name	Target	Research Area

HY-P1175

L-R4W2	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 .

HY-P10465

TRPV1-Tat	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 .

HY-P1175A

L-R4W2 TFA	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 .

HY-P1175B

L-R4W2 acetate	TRP Channel	Neurological Disease
L-R4W2 acetate is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 acetate may act as a potent analgesic .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0637

Eriodictyol 10+ Cited Publications Huazhongilexone	Structural Classification Classification of Application Fields Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids other families Flavonones Phenols Polyphenols Inflammation/Immunology Disease Research Fields Source Classification	Melanocortin Receptor TRP Channel
Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active *TRPV1* receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the *TRPV1* receptor and activating the Nrf2 signaling pathway. Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases .

HY-N0637A

(±)-Eriodictyol (±)-Huazhongilexone; Dihydroluteolin	Structural Classification Flavonoids Lawsonia inermis L. Lythraceae Flavones Plants Source Classification	Melanocortin Receptor TRP Channel
(±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active *TRPV1* receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the *TRPV1* receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases .

HY-N6962

α-Spinasterol	Structural Classification Plants Caryophyllaceae Melandrium firmum (S. et Z . ) Rohrb. Steroids	TRP Channel COX Bacterial
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 .

HY-N5084

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside	Structural Classification Flavonoids Classification of Application Fields Flavonones Other Diseases Phenols Polyphenols Saxifragaceae Plants Penthorum chinense Pursh Disease Research Fields Source Classification	TRP Channel HDAC p38 MAPK JNK ERK NF-κB TNF Receptor Interleukin Related
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a *TRPV1* antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 ⁺ T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .

HY-N7536

Voacangine	Alkaloids other families Classification of Application Fields Other Diseases Plants Disease Research Fields Indole Alkaloids Source Classification	TRP Channel
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 .

HY-N0637AR

(±)-Eriodictyol (Standard) (±)-Huazhongilexone (Standard); Dihydroluteolin (Standard)	Structural Classification Flavonoids Lawsonia inermis L. Lythraceae Flavones Plants Source Classification	Reference Standards Melanocortin Receptor TRP Channel
3-Chlorobenzoic acid (Standard) is the analytical standard of 3-Chlorobenzoic acid. This product is intended for research and analytical applications. (±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active *TRPV1* receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the *TRPV1* receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases .

Cat. No.	Product Name	Chemical Structure

HY-16935S

Mavatrep-d6
Mavatrep-d₆ (JNJ-39439335-d₆) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (K_i=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 .

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