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NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoidCB1receptor. NESS 0327 is more than 60,000-fold selective for the CB1receptor .
O-2050 is a high affinity cannabinoidCB1receptor 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 .
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 .
AM6545 is a peripherally active, cannabinoidreceptor 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 .
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 .
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 .
CB1 inverse agonist 2 is an orally active inverse agonist of CannabinoidReceptorCB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
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 .
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 .
(±)-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.
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) .
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 .
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 .
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) .
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 .
Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1(CB1)receptor extracted from patent WO 2004048317 A1 .
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 .
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.
Otenabant is a potent and selective cannabinoidreceptorCB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
Otenabant Hydrochloride is a potent and selective cannabinoidreceptorCB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoidCB1receptor, 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 .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1cannabinoidreceptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoidreceptor 2 .
Noladin ether is a potent and selective agonist of cannabinoidCB1receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception .
(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
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoidreceptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM) .
NIDA-41020 is a potent and selective cannabinoidreceptor1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET) .
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1(CB1)receptor inverse agonist.
Leelamine is a weak agonist of cannabinoidreceptorsCB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity .
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 .
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).
AZD1940 is an orally active, high affinity cannabinoidCB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action .
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1receptor, 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 .
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 cannabinoidCB1receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats.
, and displays efficacy as a feeding inhibitor .
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptorCB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
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.
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) .
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 CB1receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist .
ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoidreceptorCB1. 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 CB1cannabinoidreceptors, acting as a partial agonist. CB-25 enhances Forskolin (HY-15371)-induced cAMP formation in cancer cells but not hCB1-CHO cells .
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 .
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 .
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 .
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 .
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 CB1receptors .
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 .
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).
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
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].
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 .
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 .
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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].
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 .
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 .
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 .
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].
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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].
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 .
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 .
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 .
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.
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 .
(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 .
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 .
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 .
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 .
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 .
ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoidreceptorCB1. 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 .
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1cannabinoidreceptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoidreceptor 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 CB1cannabinoidreceptors. 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 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 .
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoidreceptorCB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119 .
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) .
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 CB1receptor. 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 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 .
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
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].
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 .
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.
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).
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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].
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].
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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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 cannabinoidCB1receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1receptors. 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].