84 Results for "

TRPV1 antagonist

" in MedChemExpress (MCE) Product Catalog:
Products (84)

84 Results for "TRPV1 antagonist" in MCE Product Catalog:

65
65 Publications Verification
Cat. No.: HY-15640
CAS No.: 138977-28-3
Purity:  98.14%
Target:  

TRP Channel Apoptosis

Research Areas:  

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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16
16 Cited Publications
Cat. No.: HY-N0637
CAS No.: 552-58-9
Synonyms: Huazhongilexone
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 .
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11
11 Cited Publications
Cat. No.: HY-101736
CAS No.: 545395-94-6
Purity:  99.76%
Target:  

TRP Channel

Research Areas:  

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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9
9 Cited Publications
Cat. No.: HY-18662
CAS No.: 1254205-52-1
Target:  

TRP Channel

Research Areas:  

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 .
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8
8 Cited Publications
Cat. No.: HY-10634
CAS No.: 659730-32-2
Purity:  99.97%
Target:  

TRP Channel

Research Areas:  

Neurological Disease

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
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8
8 Cited Publications
Cat. No.: HY-12245
CAS No.: 472981-92-3
Purity:  98.11%
Target:  

TRP Channel

Research Areas:  

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 .
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8
8 Cited Publications
Cat. No.: HY-10633
CAS No.: 501951-42-4
Purity:  99.98%
Target:  

TRP Channel

Research Areas:  

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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5
5 Cited Publications
Cat. No.: HY-19960
CAS No.: 393514-24-4
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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4
4 Cited Publications
Cat. No.: HY-107436
CAS No.: 155877-83-1
Purity:  ≥99.0%
Target:  

RAR/RXR TRP Channel

Research Areas:  

Neurological Disease Cancer

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 .
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2
2 Cited Publications
Cat. No.: HY-12195
CAS No.: 460746-46-7
Purity:  99.23%
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
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2
2 Cited Publications
Cat. No.: HY-105285
CAS No.: 946846-83-9
Purity:  99.54%
Synonyms: Neu-P11
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 .
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2
2 Cited Publications
Cat. No.: HY-12428
CAS No.: 1221443-94-2
Purity:  99.92%
Target:  

TRP Channel

Research Areas:  

Neurological Disease

A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
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1
1 Cited Publications
Cat. No.: HY-12777
CAS No.: 1005168-10-4
Purity:  95.76%
Synonyms: PAC-14028
Target:  

TRP Channel

Research Areas:  

Inflammation/Immunology

Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
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1
1 Cited Publications
Cat. No.: HY-N5084
CAS No.: 205370-59-8
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 .
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1
1 Cited Publications
Cat. No.: HY-100129
CAS No.: 821768-06-3
Purity:  99.94%
Target:  

TRP Channel

Research Areas:  

Neurological Disease

JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine .
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1
1 Cited Publications
Cat. No.: HY-160900
CAS No.: 1803003-65-7
Target:  

TRP Channel

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-104059
CAS No.: 1470018-52-0
Purity:  99.89%
Target:  

TRP Channel

AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research .
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Cat. No.: HY-N0637A
CAS No.: 4049-38-1
Synonyms: (±)-Huazhongilexone; Dihydroluteolin
(±)-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 .
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Cat. No.: HY-144372
CAS No.: 2765294-54-8
Purity:  99.30%
Target:  

TRP Channel

Research Areas:  

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 .
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Cat. No.: HY-16935
CAS No.: 956274-94-5
Synonyms: JNJ-39439335
Target:  

TRP Channel

Research Areas:  

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 .
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