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NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor .
Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoidreceptor type 1 (CB1) with an IC50 value of 8.92 µM .
MDMB-FUBICA, a synthetic cannabinoid, is a potent agonist of the cannabinoidreceptors with psychoactive properties. MDMB-FUBICA can be used in electronic cigarette .
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoidCB1receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoidreceptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
O-2050 is a high affinity cannabinoid CB1receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice .
BB-22 is a cannabinoid wih dopamine (DA) stimulant properties. BB-22 shows affinity to CB1 receptors with a Ki value of 0.11 nM and an EC50 value of 2.9 nM .
CBR Agonist-1 (27a-cis) is a cannabinoidreceptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases .
Lixosicone is a signaling-specific inhibitor of the cannabinoidreceptor 1 (CB1-SSi). Lixosicone plays an important role in Cannabis use disorder (CUD) .
hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoidreceptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities .
GP1a is a potent agonist of cannabinoidreceptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization .
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
Vicasinabin (RG7774) is the potent agonist of cannabinoidreceptor 2 (CB2). Vicasinabin has the potential for the research of human diseases including chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and other related diseases (extracted from patent US20130116236A1) .
AM8936 acts as a balanced and potent cannabinoidreceptor type-1 (CB1) agonist in functional assays (EC50s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits high affinity for rat CB1 (rCB1) with Ki of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc .
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoidreceptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM .
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoidreceptor type 1 (CB1) ligand (Ki=4.9 μM) .
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoidreceptorsCB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells .
Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoidreceptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .
(±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
Anandamide (AEA) is an endogenous cannabinoid that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. The biological actions of AEA are terminated by cellular uptake and hydrolysis of the amide bond by the enzyme fatty acid amide hydrolase. Arachidonoyl-N-methyl amide is an analog of anandamide that binds to the human central cannabinoid (CB1) receptor with a Ki of 60 nM. It inhibits rat glial gap junction cell-cell communication 100% at a concentration of 50 μM.
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoidreceptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoidreceptor 2 .
Anandamide (AEA) is an endogenous cannabinoid that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. The biological actions of AEA are terminated by cellular uptake and hydrolysis of the amide bond by the enzyme fatty acid amide hydrolase. Arachidonoyl-N,N-dimethyl amide is an analog of anandamide that exhibits weak or no binding to the human central cannabinoid (CB1) receptor (Ki >1 μM). It inhibits rat glial gap junction cell-cell communication 100% at a concentration of 50 μM.
Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1 .
R-2 Methanandamide (Compound 2) is a cannabinoid Anandamide (HY-10863) analog with a Ki of 119 nM for the cannabinoidreceptor (Ki is determined using rat brain membranes with PMSF) .
PF-514273 is an orally active, selective antagonist for cannabinoid-1receptor (CB1) with IC50 of 1 nM. PF-514273 reduces the food uptake in mice, and can be used for obesity research .
Docosatetraenylethanolamide (DEA) is a cannabinoidreceptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system .
1'-Naphthoyl-2-methylindole (Compound 88) is a cannabinoid mimetics and an inhibitor for Win 55212-2, that inhibits 34% of [3H]Win 55212-2 binding to cannabinoidreceptors at 3 μM .
Dihomo-γ-Linolenoyl Ethanolamide, an endocannabinoid, is a cannabinoid (CB) receptor agonist with Kis of 857 nM and 598 nM for human recombinant CB1 and CB2 receptors, respectively .
ART26.12 is an orally active FABP5 inhibitor with anti-cannabinoid properties. ART26.12 effectively prevents and alleviates Oxaliplatin (HY-17371)-induced pain through lipid modulation and cannabinoidreceptor activation .
Otenabant Hydrochloride is a potent and selective cannabinoidreceptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
Otenabant is a potent and selective cannabinoidreceptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2 .
CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity .
APP-FUBINACA is a cannabinoidreceptor agonist and a derivative of phenylalaninamide-based indazole-3-carboxamide. APP-FUBINACA exhibits neurostimulatory effects .
L759633 is a potent and selective agonist of cannabinoidreceptor (CB2)receptor, with Kis of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production .
Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) .
AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoidreceptor availability . AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CB1R agonist 1 (Compound '1350') is a potent full agonist of the cannabinoid-1 receptor (CB1R), with a Ki value of 0.95 nM. CB1R agonist 1 exhibits significant pain-reducing effects in multiple pain models, including acute heat pain, inflammatory pain, and neuropathic pain .
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoidreceptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively .
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoidreceptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM) .
(R)-SLV 319 is a potent and selective cannabinoidreceptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319
Noladin ether is a potent and selective agonist of cannabinoid CB1receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception .
20-HETE Ethanolamide is a metabolite of endocannabinoid Anandamide. 20-HETE Ethanolamide binds to the rat brain cannabinoid CB1 receptor with a Ki of 985 nM .
Arachidonoyl ethanolamide phosphate, an endocannabinoid, is an endogenous ligand for cannabinoidreceptors in the central nervous system (CB1 subtype) and peripheral immune cells (CB2 subtype) .
Surinabant (SR 147778) is an orally active, selective cannabinoidreceptor type 1 CB1R antagonist. Surinabant is used in studies of obesity and alcoholism .
Rosonabant is a selective antagonist for cannabinoidreceptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder .
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoidreceptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
MDA7 is the selective agonist for cannabinoidreceptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models .
PF-03550096 is an orally active synthetic cannabinoid (CB) that selectively targets peripheral CB2receptors with a Ki value of 7.9 nM. PF-03550096 has analgesic activity .
AB-FUBINACA 3-fluorobenzyl isomer is a synthetic cannabinoid that belongs to the indole derivatives and has a high affinity for the central CB1receptors (Ki= 0.9 nM), exhibiting anticonvulsant activity .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1receptor and an agonist of CB2receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases .
BAY 38-7271 is selective and highly potent and cannabinoidCB1/CB2receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1receptor and CB2receptor, respectively. BAY 38-7271 has strong neuroprotective properties .
SMM-189 is a potent and selective cannabinoidreceptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research .
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with a Ki of 6.3 nM. SER-601 has analgesic and antidiabetic properties and can be used for relevant research .
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors .
HU 433 is a synthetic cannabinoidCB2receptor agonist and is the enantiomer of HU 308 (HY-161510). HU 433 exerts its anti-inflammatory and neuroprotective effects by binding to CB2receptors. HU 433 can be used in the study of neuroinflammation and retinal diseases .
Bay 59-3074 is a selective cannabinoidCB1/CB2receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2receptors, respectively. Bay 59-3074 has analgesic properties .
Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoidreceptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Virodhamine TFA is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1receptor and an agonist of CB2receptor. Virodhamine TFA induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine TFA can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases .
Yangonin (Standard) is the analytical standard of Yangonin. This product is intended for research and analytical applications. Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
JTE 7-31 selectively acts on peripheral cannabinoidreceptors, minimizing central nervous system side effects. They exhibit potent immunomodulatory, anti-inflammatory and anti-allergic properties, as well as inhibitory effects on nephritis .
CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells .
NIDA-41020 is a potent and selective cannabinoidreceptor 1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET) .
CB2 receptor agonist 3 is a robust and selective CB2cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells .
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoidreceptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
LH-21 is a potent in vivo neutral cannabinoidCB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats.
, and displays efficacy as a feeding inhibitor .
MDA 19 is a potent and selective agonist of human cannabinoidreceptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
VIP36 is an agonist of cannabinoidreceptor type 1 (CB1) and has analgesic activity. VIP36 exerts its analgesic activity by reducing the recruitment of arrestin proteins and can be used for research in the field of chronic pain .
CB1 antagonist 4 is a inverse agonist of cannabinoidreceptor 1 (CB1) with an IC50 of 0.4 nM. CB1 antagonist 4 can reduce body weight, improve plasma inflammatory markers and glucose homeostasis .
CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoidreceptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model .
AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC50s of 45.71 and 0.076 nM, respectively.
CB1 inverse agonist 2 is an orally active inverse agonist of CannabinoidReceptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
exo-Tetrahydrocannabivarin (Compound 12) is a Δ 9,11-THC analogue. exo-Tetrahydrocannabivarin weakly binds to cannabinoidreceptors (CB) (IC50: 1.4 μM). exo-Tetrahydrocannabivarin is active on both motor and analgesic aspects in mice .
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoidCB1receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
BNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding .
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoidreceptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis [2,3].
ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoidreceptor CB1. It is a chemical that affects the endocannabinoid system in the body, which regulates various physiological processes such as appetite, pain perception, mood, and memory .
(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoidreceptor type 1 (CB1R)/iNOS antagonist, with a Ki of 5.7 nM for CB1R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis .
OMDM169 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor with activity to increase 2-AG levels. OMDM169 exerts analgesic activity through indirect activation of cannabinoidreceptors. The effective concentration of OMDM169 is 0.13 μM .
AZD-2207 is a cannabinoidreceptorCB1 antagonist, known for its high lipophilicity. AZD-2207 has good intestinal permeability in the Caco-2 model and can be used in research related to type 2 diabetes and obesity .
CB-25 is a ligand of CB1cannabinoidreceptors, acting as a partial agonist. CB-25 enhances Forskolin (HY-15371)-induced cAMP formation in cancer cells but not hCB1-CHO cells .
PSB-KD107 is an agonist of the cannabinoid activated orphan G-protein-coupled receptorGPR18, and PSB-KD107 has anti-inflammatory activity. PSB-KD107 can be used in the study of Duchenne muscular dystrophy .
Cannabidiorcol (CBDO, CBD-C1, O-1821) is related to cannabidiol, with the pentyl side chain shortened to a methyl group. Cannabidiorcol has low affinity for cannabinoidreceptors (CBs) and is an agonist of the transient receptor potential channel (TRP channel), through which it produces antiinflammatory effects, but can also promote tumorigenesis at high concentrations .
CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoidreceptor type 1 (CB1)receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects .
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoidreceptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
GW-405833 (L768242) is a potent, selective cannabinoidreceptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain .
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoidreceptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
RNB-61 is an oral active agonist of cannabinoid CB2 receptor (CB2R), with the Ki ranging from 0.13 nM to 1.81 nM. RNB-61 has nephroprotective and/or antifibrotic effects. RNB-61 has negligible penetration into the brain .
Flavoglaucin is a compound that exhibits significant anti-tumor promoting activity. Flavoglaucin exhibits significant inhibition of PTP1B with an IC50 value of 13.4 micromolar. Flavoglaucin also shows good binding affinity to human opioid or cannabinoidreceptors. Flavoglaucin has anti-inflammatory activity .
KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research .
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoidreceptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
GW-405833 (L768242) hydrochloride is a potent, selective cannabinoidreceptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 hydrochloride also behaves as a noncompetitive CB1 antagonist. GW-405833 hydrochloride suppresses inflammatory and neuropathic pain .
(R)-Zevaquenabant ((R)-MRI-1867) is the enantiomer of Zevaquenabant (HY-141411A). Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoidCB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD) .
Rimonabant (Hydrochloride) (Standard) is the analytical standard of Rimonabant (Hydrochloride). This product is intended for research and analytical applications. Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoidreceptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Delta8-THC acetate (Delta8-tetrahydrocannabinol) is a psychoactive phytocannabinoid, that binds to cannabinoidreceptor 1 (CB1 receptor), and exhibits anti-nausea, appetite-stimulating, and anti-inflammatory activities. Delta8-THC acetate exhibits probably neuroprotective efficacy and can be used in anti-anxiety and antidepressant research .
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoidreceptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1cannabinoidreceptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action .
Δ8-THCP (Δ8-Tetrahydrocannabiphorol; n-Heptyl Δ8-THC) (Compound 1a) is a semisynthetic cannabinoid that serves as an analytical reference standard and exhibits affinity for the CB1receptor .
Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic .
AB-FUBICA (Compound 13) is a CB1 and CB2receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC50 values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms .
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
MDA 19 (Standard) is the analytical standard of MDA 19. This product is intended for research and analytical applications. MDA 19 is a potent and selective agonist of human cannabinoidreceptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
Glycerophospho-N-Arachidonoyl Ethanolamine is a N-acylated ethanolamines (NAEs). Most NAEs are naturally occurring lipids with diverse biological activities. Different types of NAE can be derived from glycerophosphate-linked precursors through the activity of glycerophosphodiesterase 1 (GDE1). Glycerophosphate-N-Arachidonoyl Ethanolamine is the precursor of Anandamide (AEA), also known as Anandamide. AEA is an endocannabinoid neurotransmitter that binds to central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM compared to 46 nM for δ9-THC.
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone (compound 45) is a potential inhibitor of fatty acid amide hydrolase (FAAH) (pI50: 5.89) and is active against CB(1) and CB(2) ) Lack of affinity for cannabinoidreceptors .
O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoidreceptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels .
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoidreceptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .
Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoidreceptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoidreceptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM .
2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
URB447 is a peripherally restricted CB1cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity .
S-777469 is a selective and orally available cannabinoid type 2 receptor(CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoidreceptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
CB1R Allosteric modulator 5 (compound 3) is a selective, and blood-brain barrier (BBB) permeable Cannabinoidreceptor type 1 allosteric modulator with a pIC50 of 6.89. CB1R Allosteric modulator 5 attenuates both cocaine-seeking behavior specific to cue-induced reinstatement and cocaine-induced behavioral sensitization without altering locomotor activity .
Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoidreceptorsCB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoidreceptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1)receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication . Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoidreceptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
CB2R agonist 1 is a selective ligand of cannabinoidreceptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation .
Pregnenolone (Standard) is the analytical standard of Pregnenolone. This product is intended for research and analytical applications. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant[1][2].
Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoidreceptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
ABD459 is a CB1receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders .
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines .
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoidreceptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders .
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.
MCE provides a unique collection of 2,968 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.
ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoidreceptor CB1. It is a chemical that affects the endocannabinoid system in the body, which regulates various physiological processes such as appetite, pain perception, mood, and memory .
Glycerophospho-N-Arachidonoyl Ethanolamine is a N-acylated ethanolamines (NAEs). Most NAEs are naturally occurring lipids with diverse biological activities. Different types of NAE can be derived from glycerophosphate-linked precursors through the activity of glycerophosphodiesterase 1 (GDE1). Glycerophosphate-N-Arachidonoyl Ethanolamine is the precursor of Anandamide (AEA), also known as Anandamide. AEA is an endocannabinoid neurotransmitter that binds to central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM compared to 46 nM for δ9-THC.
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoidreceptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoidreceptor 2 .
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1cannabinoidreceptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1receptor and an agonist of CB2receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases .
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoidreceptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM .
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoidreceptor type 1 (CB1) ligand (Ki=4.9 μM) .
Docosatetraenylethanolamide (DEA) is a cannabinoidreceptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system .
Dihomo-γ-Linolenoyl Ethanolamide, an endocannabinoid, is a cannabinoid (CB) receptor agonist with Kis of 857 nM and 598 nM for human recombinant CB1 and CB2 receptors, respectively .
20-HETE Ethanolamide is a metabolite of endocannabinoid Anandamide. 20-HETE Ethanolamide binds to the rat brain cannabinoid CB1 receptor with a Ki of 985 nM .
Yangonin (Standard) is the analytical standard of Yangonin. This product is intended for research and analytical applications. Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoidreceptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis [2,3].
Flavoglaucin is a compound that exhibits significant anti-tumor promoting activity. Flavoglaucin exhibits significant inhibition of PTP1B with an IC50 value of 13.4 micromolar. Flavoglaucin also shows good binding affinity to human opioid or cannabinoidreceptors. Flavoglaucin has anti-inflammatory activity .
Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoidreceptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoidreceptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoidreceptorsCB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication . Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Pregnenolone (Standard) is the analytical standard of Pregnenolone. This product is intended for research and analytical applications. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoidreceptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoidreceptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders .
CNR2 Protein-VLP, Human (HEK293) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P702775. May have binding signals with Anti-His antibodies.
CNR1 Protein-VLP, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.
CNR2 Protein-VLP, a heterotrimeric G protein-coupled receptor, crucially inhibits adenylate cyclase, mediating functions in inflammatory responses, nociceptive transmission, and bone homeostasis. Its modulation of cellular signaling underscores its significance in physiological processes, positioning CNR2 Protein-VLP as a key regulator in inflammatory, sensory mechanisms, and bone equilibrium. CNR2 Protein, Human (Cell-Free, His) is the recombinant human-derived CNR2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag.
CNR2 Protein-VLP, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant[1][2].
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoidreceptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoidreceptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoidreceptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoidreceptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis .
Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoidreceptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Phospho-Cannabinoid Receptor I (Ser316) Antibody (YA2350) is a non-conjugated IgG antibody, targeting Phospho-Cannabinoid Receptor I (Ser316), with a predicted molecular weight of 53 kDa (observed band size: 53 kDa). Phospho-Cannabinoid Receptor I (Ser316) Antibody (YA2350) can be used for WB experiment in human background.
CB1 Antibody is a rabbit-derived non-conjugated IgG antibody, targeting CB1, with a predicted molecular weight of 52 kDa (observed band size: 52 kDa). CB1 Antibody can be used for WB, IHC-P, IHC-F, ICC/IF, ELISA experiments in human, rat backgrounds.
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoidreceptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
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