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I9281 5′-Iodoresiniferatoxin solid Vanilloid receptor antagonist.
I7033 6′-Iodoresiniferatoxin amorphous semi-solid VR1 vanilloid receptor partial agonist.
I0909 6-Iodonordihydrocapsaicin ≥98% (HPLC), solid TRPV1 (V1) vanilloid receptor antagonist.
A2731 AMG 9810 ≥98% (HPLC), powder AMG 9810 is a potent, non-vanilloid, antagonist of the TRPV1 receptor. IC50 = 17 nM.
SML0103 AMTB hydrate ≥98% (HPLC) AMTB is a TRPM8-selective antagonist with no cross reactivity to TRPV1 or 4. The pIC50 of icilin activation of TRPM8 is 6.23 i.v. administration of AMTB reduced the frequency of rhythmic contractions in volume-loaded bladder and inhibited blood pressure and visceromotor reflex responses to bladder distention.
SML0395 Ac-EEMQRR-NH2 trifluoroacetate salt ≥95% (HPLC) Ac-EEMQRR-NH2 is a SNAP25 N-terminal-derived peptide that inhibits the SNARE complex and possibly blocks neuronal exocytosis. Ac-EEMQRR-NH2 exhibits anti-inflammatory and anti-wrinkle activity. It is used as anti-wrinkle cosmetics ingredient.
SML0520 Arvanil ≥98% (HPLC), solution (in ethanol) Arvanil is an activator of cannabinoid and vanilloid receptors, and a potent inhibitor of anandamide accumulation. Arvanil inhibits growth of astrocytoma xenograft tumors in mice, mimicing the effect of neural precursor cells, that have been shown to kill TRPV1-expressing tumor cells by secreting endovanilloids.
SML0355 BCTC ≥98% (HPLC) BCTC is a potent antagonist of the vanilloid receptor TRPV1. BCTC blocks capsaicin-induced contractions in a variety of smooth muscle tissues, including guinea pig ileum, bladder and trachea with no effects on capsaicin-sensitive, sensory neuron-mediated positive inotropy. The compound penetrates the CNS and has strong analgesic properties.
M2028 Capsaicin ≥95%, from Capsicum sp. Prototype vanilloid receptor agonist. Neurotoxin; activates sensory neurons that give rise to unmyelinated C-fibers, many of which contain substance P. Topical application desensitizes the sensory nerve endings giving a paradoxical antinociceptive effect; systemic administration can be neurotoxic to capsaicin-sensitive cells, especially in newborn animals. Active component of chili peppers.
C191 Capsazepine ≥98% (HPLC), solid Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin.
M1022 Dihydrocapsaicin from Capsicum sp., ≥85% VR1 vanilloid receptor agonist.
G0798 GSK1016790A ≥98% (HPLC) GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).
SML0942   GSK2193874 ≥98% (HPLC) GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.
SML0143 HC-067047 ≥98% (HPLC) HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively.
I9532 Icilin ≥97% (HPLC), solid Icilin is a potent agonist at the CMR1 cold- and menthol-sensitive receptor.
I1279 Isovelleral solid Vanilloid receptor agonist.
J3580 JNJ 17203212 ≥98% (HPLC) JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist that does not inhibit related TRP channels such as TRPV2, TRPV4, or TRPA1. Listed in BJP with IC50= 65 nM. TRPV1 channels are activated by heat, capsaicin and the endocannabinoid anandamide. Interest in TRPV1 antagonists in the transmission and modulation of pain.
SML0893   M8-B hydrochloride ≥98% (HPLC) M8-B is a selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. M8-B blocked cold-induced and icilin or methol-induced activation of rat, human, and murine TRPM8 channels with IC50 values in rat ranging from 7.8 nM to 64.3 nM, and it did not block other TRP channels (IC50 values > 20 mM). M8-B decreased deep body temperature in both mice and rats, showing that blockade of TRPM8 receptor might be used to induce therapeutic hypothermia, an effective treatment in cardiac arrest.
SML1623 MSP-3 ≥98% (HPLC) MSP-3 is a Transient Receptor Potential Vanilloid Type-1 (TRPV1) channel agonist with antioxidant and neuroprotective activity. MSP-3 activated TRPV1 channels with similar efficacy as compared to capsaicin (EC50 = 870 nM). It protected a keratinocyte cell line from oxidative stress damage with more efficacy than capsaicin and prevented the damage caused by H2O2 in differentiated human neuroblastoma cell lines as well as in rat cortical slices.
SML1488   Metamizole sodium hydrate ≥98% (HPLC) Metamizole (Dipyrone) is a potent analgesic and antipyretic. Metamizole inhibits prostaglandin synthesis in both the periphery and the central nervous system. Metamizole may act as a prodrug. It is rapidly hydrolyzed to N-methyl-4-aminoantipyrine (MAA) and 4-aminoantipyrine (AA) which inhibit cyclo-oxygenase activity and can be further acylated with arachidonic acid forming compounds that bind to central and peripheral cannabinoid (CB1 and CB2) receptors and TRPV1 receptors. It is believed that these metabolites play a major role in metamizole activity. Metamizole has been withdrawn from clinical use in several countries because of a side-effect of agranulocytosis in some patients.
V9130 N-Vanillylnonanamide ≥97%, powder  
O2389 OMDM-1 ≥97% (HPLC), powder Potent, selective inhibitor of anadamide cellular uptake with low affinity for CB1 and CB2 receptors, no activity at VR1 receptor or fatty acid amide hydrolase (FAAH); stable to enzymatic hydrolysis by rat brain homogenates.
O0257 Olvanil powder Vanilloid receptor agonist
PZ0245   PF-05105679 ≥98% (HPLC) PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
P9983 Phorbol 12,13-didecanoate 20-homovanillate ≥98% Resiniferatoxin-type vanilloid phorbol ester with capsaicin-like selectivity for the vanilloid receptor.
P266 Phorbol 12-phenylacetate 13-acetate 20-homovanillate solid Vanilloid receptor agonist.
R0658 RN-1734 ≥98% (HPLC) RN-1734 is a selective TRPV4 antagonist.
SML1547 RN-9893 ≥98% (HPLC) RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
SML1602 RQ-00203078 ≥98% (HPLC) RQ-00203078 is an orally available potent and selective TRPM8 antagonist that potently reduces cation currents induced by menthol and other TRPM8 agonists. RQ-00203078 inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
R8756 Resiniferatoxin from Euphorbia poisonii, ~95% Potent VR1 vanilloid receptor agonist that has been used to label the vanilloid receptor in sensory ganglia; activates protein kinase C. Diterpene ester that is related to phorbol, but is not tumorigenic.
SML1600   Rinvanil ≥98% (HPLC) Rinvanil is a Capsaicin analogue that potently activates transient receptor potential vanilloid 1 (TRPV1) channels. Rinvanil induces neuroprotective mild hypothermia in ischemic brain injured mice through TRPV1 activation. Rinvanil exhibits potent anticancer activity in cancer cell lines including cervical (HeLa, CaSKi, ViBo) and leukemia (P388, J774, WEHI-3) cell lines. Rinvanil is not cytotoxic to normal lymphocytes.
TRPV1 (transient receptor potential vanilloid 1) is a capsaicin receptor. It is strongly expressed in sensory neurons and participates in pain perception. In brain, it regulates neuronal function, motor behaviour and neuroinflammation. Capsaicin plays an important role in the activation of TRPV1.
SML0890   SB 452533 ≥98% (HPLC) SB-452533 acts as a competitive inhibitor at the capsaicin binding site on the transient receptor potential channel TRPV1 receptor with a pKb of 7.7 versus capsaicin and pIC50 of 7.0 versus pH. At higher concentrations, SB-452533 is also active at TRPM8 with an IC50 of 571 nM. It has a high clearance rate, so is not suitable for in vivo use.
S0441 SB-366791 ≥98% (HPLC), powder Vanilloid receptor-1 (TRPV1) antagonist.