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- Cat. No.
- A22264
A 784168
A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1).
In stock View Details -
- Cat. No.
- A22607
M8-B (hydrochloride)
M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively).
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- Cat. No.
- A22608
LASSBio-1135
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.
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- Cat. No.
- A26088
TRPV1 antagonist 10
TRPV1 Antagonist 10 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 33.06 nM. This compound also demonstrates moderate inhibition of URAT1 (IC50 = 22.51 μM) and partial inhibition of GLUT9 (60.25% at 50 μM). TRPV1 Antagonist 10 is valuable in research applications focusing on analgesia and the management of hyperuricemia, making it a significant tool for studying inflammatory pain mechanisms.
Out of stock
All 3 sizes -
- Cat. No.
- A27004
Pellitorine
Pellitorine is a natural amide compound that functions as a TRPV1 antagonist, effectively inhibiting pain signal transmission activated by capsaicin. This compound demonstrates significant biological activity by improving cognitive function through the upregulation of BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. In addition, Pellitorine exhibits anti-inflammatory properties by reducing the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Furthermore, it has antithrombotic effects, mitigates lipid peroxidation, and has exhibited activity against Aedes aegypti mosquito larvae as well as certain cancer types and bacteria, making it a versatile tool in chemical research applications.
In stock View Details -
- Cat. No.
- A33012
DWP-05195
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer.
Out of stock
All 3 sizes -
- Cat. No.
- A59259
CB2 receptor antagonist 1
CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways.
In stock View Details -
- Cat. No.
- A61648
(±)-Eriodictyol ((±)-Huazhongilexone, Dihydroluteolin)
Synonyms: (±)-Huazhongilexone; Dihydroluteolin
(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels.
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- Cat. No.
- A62324
Naltriben mesylate
Naltriben mesylate is a potent antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It demonstrates high affinity, with Ki values of 0.013 nM for the δ receptor, alongside 19 nM and 152 nM for μ and κ receptors, respectively. Research indicates that Naltriben mesylate enhances glioblastoma cell migration and invasion, making it a valuable tool for studies related to neurological diseases and cancer biology.
Out of stock
All 1 sizes -
- Cat. No.
- A62558
TRPV1 antagonist 11
TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research.
In stock View Details -
- Cat. No.
- A62615
Naltriben
Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas.
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- Cat. No.
- A66070
A-425619
A-425619 is a selective antagonist of the transient receptor potential type V1 (TRPV1), exhibiting oral bioactivity. It effectively inhibits capsaicin- and N-arachidonoyl-dopamine (NADA)-induced calcium influx in both dorsal root ganglia and trigeminal ganglia. A-425619 demonstrates efficacy in alleviating pathophysiological pain linked to inflammation and tissue injury in preclinical models. This compound is valuable for researching pain mechanisms associated with inflammatory conditions.
In stock View Details -
- Cat. No.
- A68685
ADM 12
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain.
Out of stock
All 3 sizes -
- Cat. No.
- A68690
BI-749327
BI-749327 is a potent and highly selective antagonist of the TRPC6 channel, exhibiting IC50 values of 13 nM for mouse TRPC6, 19 nM for human TRPC6, and 15 nM for guinea pig TRPC6. This compound demonstrates an 85-fold selectivity for mouse TRPC6 over TRPC3 and a 42-fold selectivity over TRPC7. Due to its oral bioavailability and inhibition of TRPC6, BI-749327 is suitable for research applications involving ion channel modulation and the investigation of associated physiological and pathological processes.
In stock View Details -
- Cat. No.
- A68692
SET2
SET2 is a selective antagonist of the TRPV2 channel, with an IC50 value of 0.46 μM. This compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. Additionally, SET2 diminishes lysophosphatidic acid (LPA)-induced increases in cytoplasmic calcium levels, making it useful for research focused on cancer biology and calcium signaling pathways.
In stock View Details -
- Cat. No.
- A68693
GSK205
GSK205 is a selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4) channel, exhibiting an IC50 of 4.19 μM for TRPV4-mediated calcium influx inhibition. This compound is instrumental in studying TRPV4's role in various physiological and pathological processes, including pain sensation, inflammation, and cellular mechanotransduction. GSK205 is a valuable tool for researchers investigating the therapeutic potential of TRPV4 modulation in various disease models.
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- Cat. No.
- A68695
AMTB hydrochloride
AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research.
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- Cat. No.
- A68699
LE135
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts.
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- Cat. No.
- A68711
SOR-C13
SOR-C13 is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel implicated in malignancy and poor prognosis in breast cancer. This compound exhibits significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development.
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- Cat. No.
- A68712
PF-05105679
PF-05105679 is a selective antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting an IC50 of 103 nM. This compound demonstrates promising biological activity in modulating cold-related pain pathways. It is suitable for research applications investigating the role of TRPM8 in nociception and pain management strategies.
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- Cat. No.
- A68717
Asivatrep
Synonyms: PAC-14028
Asivatrep (PAC-14028) is a potent and selective antagonist of the transient receptor potential vanilloid type I (TRPV1) channel. This compound exhibits significant analgesic effects by blocking TRPV1, which is involved in the transmission of nociceptive signals. Asivatrep is primarily utilized in research related to pain management and neurobiology. Its selective inhibition offers a valuable tool for studying TRPV1-mediated pathways and their role in various physiological and pathological conditions.
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- Cat. No.
- A68726
Elismetrep
Synonyms: MT-8554
Elismetrep (MT-8554) is a selective TRPM8 antagonist that inhibits the activity of the transient receptor potential melastatin 8 channel. It is shown to reduce the frequency of vasomotor symptoms and is valuable for research in pain modulation and sensory perception. Elismetrep offers potential applications in the study of disorders related to thermal sensation and nociception.
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- Cat. No.
- A68727
TRPV1 antagonist 3
TRPV1 antagonist 3 (Compound 7q) is a highly effective antagonist of the TRPV1 receptor, demonstrating an IC50 of 2.66 nM against capsaicin. This compound exhibits mode-selectivity and is characterized by favorable oral bioavailability (F = 60%) as well as the ability to penetrate the central nervous system. TRPV1 antagonist 3 is valuable for research focused on pain modulation and inflammatory processes.
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- Cat. No.
- A68730
PF-05214030
PF-05214030 is a potent TRPV4 antagonist, exhibiting IC50 values of 4 nM for human TRPV4 and 27 nM for rat TRPV4. This compound effectively counteracts the decrease in bladder capacity induced by intravesical administration of a TRPV4 agonist. PF-05214030 is therefore a valuable tool for investigating the role of TRPV4 in bladder physiology and may hold potential for therapeutic applications in bladder dysfunction research.
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