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CB2receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2receptor agonist 2 has high affinity and selectivity for CB2 .
CB2receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells .
CB2receptor agonist 6 (compound 70) is an agonist of CB2R, with EC50 of 162 nM. The IC50 values of CB2receptor agonist 6 are 4.83 μM for CB1R and 0.88 μM for CB2R.
CB2receptor agonist 6 is a neuroprotective agent that can be used for the reseach of neurological disease .
CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptorCB2R with Kd=39 nM. CB2receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
CB2receptor antagonist 2 (compound 39) is a potent antagonist of CB2 with an IC50 value of 0.33 μM. CB2receptor antagonist 2 has strong interactions with L17, W6.48, V6.51, and C7.42 .
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.
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 .
GW-405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 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 .
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 .
L759633 is a potent and selective agonist of cannabinoid receptor(CB2)receptor, with Kis of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production .
Bay 59-3074 is a selective cannabinoid CB1/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 .
BAY 38-7271 is selective and highly potent and cannabinoid CB1/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 .
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) .
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
HU 433 is a synthetic cannabinoid CB2receptor 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 .
LEI-101 free base is a selective and orally bioavailable CB2receptor agonist with the potential to inhibit diseases associated with inflammation and/or oxidative stress. LEI-101 free base has a binding potency to CB2receptors that is approximately 100 times higher than that to CB1 receptors. Its pEC50 value on CB2receptors is 8, while its pKi value on hERG is less than 4. LEI-101 may have an inhibitory effect on conditions such as kidney disease .
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2receptor 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 CB2receptors than to CB1 receptors .
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 .
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 CB2receptor. COR170 can be used for the research of inflammation and neuroprotection .
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 CB2receptors, respectively .
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 .
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2receptor.
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 CB2receptor.
β-Caryophyllene (Standard) is the analytical standard of β-Caryophyllene. This product is intended for research and analytical applications. β-Caryophyllene is a CB2receptor agonist.
Arachidonoyl ethanolamide phosphate, an endocannabinoid, is an endogenous ligand for cannabinoid receptors in the central nervous system (CB1 subtype) and peripheral immune cells (CB2 subtype) .
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action .
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 .
SMM-189 is a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research .
RNB-61 is an oral active agonist of cannabinoid CB2receptor(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 .
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 .
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 .
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 CB2receptors, respectively. Anorexigenic effects .
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 .
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 .
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 .
AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2receptors 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 .
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 .
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 .
KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2receptors 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 cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .
Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2receptor 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 .
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 .
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 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 .
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
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 .
CB2R/5-HT1AR agonist 1 (Compound 2o) is an orally active partial agonist of the CB2receptor (EC50=479.6 nM). CB2R/5-HT1AR agonist 1 is a full agonist of 5-HT1Areceptor (EC50=2.7 μM). CB2R/5-HT1AR agonist 1 exhibits anti-anxiety and anti-depressive effects. CB2R/5-HT1AR agonist 1 possesses favorable pharmacokinetic properties .
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/CB2receptor 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].
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
CID1172084 (compound 3) is a selective GPR55 agonist (EC50=0.16 μM). CID1172084 is more than 100-fold selective for GPR55 over GPR35, CB1, and CB2. CID1172084 can be used to further explore the biological functions and signaling pathways of the GPR55receptor .
(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM .
N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
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 cannabinoid receptorsCB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells .
URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2receptor 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 receptorsCB1 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 (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.
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.
Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (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-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1receptor. 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/CB2receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2receptors, 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 .
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
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 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 .
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (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 .
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 .
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 cannabinoid receptors of type-1（CB1）and CB2receptors, 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 .
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.
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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) .
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.
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
β-Caryophyllene (Standard) is the analytical standard of β-Caryophyllene. This product is intended for research and analytical applications. β-Caryophyllene is a CB2receptor agonist.
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 .
N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptorsCB1 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 is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (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 (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2receptors, 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 .
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 CB2receptors, respectively .
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 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 .
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) .
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.
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.
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.
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/CB2receptor 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].
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (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 cannabinoid receptors of type-1（CB1）and CB2receptors, 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 .
CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptorCB2R with Kd=39 nM. CB2receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
