vr1

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

Dihydrocapsaicin (CCRIS1589) is isolated from Capsicum fruit. Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Like capsaicin, dihydrocapsaicin is an irritant. Capsaicin is found in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain pure dihydrocapsaicin. Dihydrocapsaicin represents about 10% of the compound present in commercial preparations purporting to be pure capsaicin, but it has about the same pungency as capsaicin. VR1 (vanilloid receptor 1) is a heat activated calcium ion channel which functions as a part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. The potency of dihydrocapsaicin at VR1 appears equivalent to capsaicin. Antioxidant. Reduces oxidation of serum lipids. Mutagenic. Dihydrocapsaicin is an activator of VR1.

VR17-04, a metabolite of Enisamium, inhibits the incorporation of GTP and UTP during RNA synthesis. Its mechanism of action was elucidated through docking and molecular dynamics simulations. These findings suggest that VR17-04 could serve as a potential antiviral strategy for managing COVID-19.

VR11 aptamer is a DNA-based TNF-α inhibitor with a KD of 7.0 nM. It effectively blocks TNFα-induced apoptosis (apoptosis) and prevents NO production. VR11 aptamer demonstrates no immunogenicity as it does not trigger an immune response when administered intraperitoneally in C57BL/6 mouse models. This aptamer is suitable for research on inflammatory diseases.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

IHVR-17028 is a potent broad-spectrum ERα-glucosidase I (α-glucosidase I) inhibitor with IC50 of 0.24 μM and antiviral activity. IHVR-17028 inhibited BVDV, TCRV and DENV, and EC50 values were 0.4 μM, 0.26 μM and 0.3 μM, respectively. IHVR-17028 can be used to study infectious diseases.

IHVR-19029 is an effective endoplasmic reticulum (ER) α-glucosidases I and II inhibitor (IC50: 0.48 μM for ER a-glucosidase I). IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Ebola virus, Dengue virus, and Rift

IHVR-11029 is a potent inhibitor of ER α-glucosidase. IHVR-11029 is active against multiple hemorrhagic fever viruses and efficiently disrupts the morphogenesis of a broad spectrum of enveloped viruses.

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

OD36 hydrochloride (OD-36 hydrochloride) is a potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 hydrochloride is a macrocyclic inhibitor that binds efficiently to the ATP pocket of the ALK2 kinase and effectively antagonizes mutant ALK2 signaling and osteogenic differentiation.OD36 hydrochloride targets ALK2. OD36 hydrochloride targets ALK2 with a KD of 37 nM.

LDN-193189 Tetrahydrochloride (DM-3189 Tetrahydrochloride) is a selective inhibitor of BMP type I receptors, inhibiting ALK2 and ALK3 (IC₅₀ = 5/30 nM), with weaker activity against ALK4, ALK5, and ALK7, and can be used for research into progressive osseous fibrodysplasia.

Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid and a ligand for vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1), exhibiting neuroprotective activity, inhibiting spasm, and enhancing cisplatin chemotherapy sensitivity by inducing ferroptosis in HCC cells in vivo. It induces ferroptosis in liver cancer cells via binding to MICU1.

TRPV1 (VR1) receptor antagonist

TRPV1 (VR1) vanilloid receptor partial agonist

OLDA (N-oleoyldopamine) is an endogenous lipid modulator found in the brain and a potent TRPV1 receptor agonist (EC50 = 36 nM). It regulates nociceptive neurotransmission and thermal homeostasis at the physiological level by activating vanilloid receptors to induce intracellular calcium release.

Several different arachidonoyl amino acids, including N-arachidonoyl-L-alanine (NALA), have been isolated and characterized from bovine brain. The glycine congener (NAGly) was further characterized and found to suppress formalin-induced pain in rats. NALA may have activity at cannabinoid receptor and/or VR1, but has not been fully characterized to date.

Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.

DD-161515 is a VR1 antagonist.

SB-366791 is a new and selective cinnamide TRPV1 antagonist.

L-R4W2 TFA acts as a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), demonstrating significant inhibitory activity with an IC50 value of 0.1 μM. This compound potentially offers powerful analgesic properties [1] [2].

CEDAEVFKDSMVPGEK, the peptide sequence corresponding to the rat vanilloid receptor subtype 1 (VR1), facilitates the detection and mapping of VR1 distribution [1].

N-Arachidonoyl-L-serine (ARA-S), a recently isolated endocannabinoid with a distinct activity profile that diverges from typical endocannabinoids, does not interact with central cannabinoid (CB1), peripheral cannabinoid (CB2) receptors, or vanilloid receptor 1 (VR1). Unlike other compounds, ARA-S (5 mg/kg) counteracts the lowering of blood pressure induced by a 10 mg/kg intravenous bolus of abnormal cannabidiol (Abn-CBD) in anesthetized rat models. Additionally, akin to Abn-CBD, ARA-S induces relaxation in isolated rat mesenteric arteries and abdominal aorta and promotes phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in human umbilical vein endothelial cells (HUVEC). The mechanisms through which ARA-S and Abn-CBD exert their effects on vascular systems show variations and merit deeper investigation.