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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 .
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoidCB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice .
(R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319
CBR Agonist-1 (27a-cis) is a cannabinoid receptor (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 .
Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoid receptor type 1 (CB1) with an IC50 value of 8.92 µM .
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively .
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo .
MDA 19 is a potent and selective agonist of human cannabinoid receptor 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 .
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 .
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 .
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 .
hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities .
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
GP1a is a potent agonist of cannabinoid receptor 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 .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
Vicasinabin (RG7774) is the potent agonist of cannabinoid receptor 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 cannabinoid receptor 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 .
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 TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
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 .
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM .
AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications .
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 cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM) .
(±)-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.
Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1 .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .
GW405833 hydrochloride is a potent and selective cannabinoid-2 (CB2) receptor agonist (EC50 = 0.65 nM; maximum inhibition = 44.6%). GW405833 hydrochloride produces potent antihyperalgesic effects in several rodent models of pain .
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 .
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 cannabinoid receptor 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 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 .
Nervonoyl ethanolamide (NEA) is an endogenous cannabinoid that can act as a presynaptic and postsynaptic neuromodulator. Nervonoyl ethanolamide can also be used in the research of inflammation .
Heptadecanoyl ethanolamide is an endogenous cannabinoid. Heptadecanoyl ethanolamide is a synthetic analog of PEA which incorporates an odd-numbered (17-carbon) fatty acid chain .
2-Arachidonoylglycerol-d8 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d5 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception .
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM) .
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity .
2-Arachidonoylglycerol-d11 is deuterium labeled 2-Arachidonoylglycerol.2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system[1].
PF-03550096 is an orally active synthetic cannabinoid (CB) that selectively targets peripheral CB2 receptors with a Ki value of 7.9 nM. PF-03550096 has analgesic activity .
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.
Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
NIDA-41020 is a potent and selective cannabinoid receptor 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) .
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 .
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
CB1 antagonist 4 is a inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. CB1 antagonist 4 can reduce body weight, improve plasma inflammatory markers and glucose homeostasis .
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 Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
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 .
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.
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoidCB1 receptor. 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) .
(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoid receptor type 1 (CB1R)/iNOS antagonist, with a Ki of 5.7 nM for CB1R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis .
ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoid receptor 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 .
CB-25 is a ligand of CB1cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin (HY-15371)-induced cAMP formation in cancer cells but not hCB1-CHO cells .
Bay 59-3074 is a selective cannabinoidCB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties .
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 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 cannabinoid receptor 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 .
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
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 .
Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
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 CB1cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
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 .
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 .
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
MRL-650 (CB1 inverse agonist 1) is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects .
BAY 38-7271 is selective and highly potent and cannabinoidCB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties .
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. 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 .
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 .
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 CB1cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
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 CB1cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
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) 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 CB1cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
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 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels .
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 cannabinoid receptors .
CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor 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 .
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 .
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 .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors 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 .
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor 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].
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 .
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 .
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 .
CB2R agonist 1 is a selective ligand of cannabinoid receptor 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 .
COR170 (11u) is a selective CB2 inverse-agonist which is a 4-quinolone-3-carboxylic acid derivative with a Ki value of 3.8 nM for CB2 receptor. COR170 can be used for the research of inflammation and neuroprotection .
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 .
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 (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- 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].
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 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].
CB2 receptor agonist 6 (compound 70) is an agonist of CB2R, with EC50 of 162 nM. The IC50 values of CB2 receptor agonist 6 are 4.83 μM for CB1R and 0.88 μM for CB2R.
CB2 receptor agonist 6 is a neuroprotective agent that can be used for the reseach of neurological disease .
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 2286 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 cannabinoid receptor 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 .
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
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 CB1cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .
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 CB1cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
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 CB1cannabinoid receptors. 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 CB1cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor 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 cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM) .
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. 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 .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors 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 .
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees . Leelamine hydrochloride is a cannabinoid receptor 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].
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 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 .
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.
The CNR1 protein is a G-protein-coupled receptor for cannabinoids, including cannabinoids and endocannabinoids such as 2-AG, which mediates diverse effects on food intake, memory, and pain. It regulates mitochondrial respiration and inhibits leptin-induced ROS formation. CNR1 Protein, Rat (Cell-Free, His) is the recombinant rat-derived CNR1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CNR1 Protein, Rat (Cell-Free, His) is 473 a.a., with molecular weight of 58.9 kDa.
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.
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. The total length of CNR2 Protein, Human (Cell-Free, His) is 360 a.a., with molecular weight of 42.5 kDa.
2-Arachidonoylglycerol-d8 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d5 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d11 is deuterium labeled 2-Arachidonoylglycerol.2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system[1].
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Rimonabant-d10 (hydrochloride) is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
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].
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].
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor 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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