Cannabinoids

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M1438 (±)-2-Methylarachidonoyl-2′-fluoroethylamide ≥95%, ethanol solution An analog of arachidonylethanolamide (anandamide) that is a potent, selective CB1 cannabinoid receptor agonist. The methyl group at the C-2 position of arachidonic acid gives the compound enhanced metabolic stability. It can fully substitute for Δ9-THC in animal self-administration tests.
W102 (R)-(+)-WIN 55,212-2 mesylate salt ≥98% (HPLC) High affinity cannabinoid receptor agonist.
A6478 (R,S)-AM1241 ≥98% (HPLC), solid Selective CB2 cannabinoid receptor agonist
A8973 2-Arachidonyl glycerol ~10 mg/mL, ≥98% (HPLC) Endogenous cannabinoid receptor agonist.
A6226 AM251 >98% (HPLC), solid AM251 is a CB1 cannabinoid receptor antagonist.
A0980 AM281 ≥98% (HPLC) Potent and selective CB1 cannabinoid receptor antagonist/inverse agonist
SML1804 AM4113 ≥98% (HPLC) AM4113 is a Cannabinoid CB-1 neutral antagonist. AM4113 reduced reward and reinstatement of drug-seeking behavior, reducing cue-induced reinstatement in monkeys trained to self-administer cocaine.
SML0327 AM630 ≥90% (HPLC) AM630 is a selective CB2 cannabinoid antagonist/inverse agonist (Ki = 31.2 nM) with > 150-fold selectivity over CB1 receptors.
A1987 AM6545 ≥98% (HPLC) AM6545 is a peripheral CB1 cannabinoid receptor antagonist and appetite suppressant.
SML0452 AZ513 ≥98% (HPLC) AZ513 is a reversible, noncompetitive FAAH inhibitor. It also binds non-competitively at a site distinct from the catalytic site. AZ513 is 20-fold more potent against rat FAAH (IC50 27 nM) than the human form (IC50 551 nM).
A8848 Arachidonoyl dopamine ≥98% (HPLC), ethanol solution AA-DA competitively inhibits fatty acid amide hydrolase (IC50 = approx. 22 μM) from N18TG2 neuroblastoma cells and inhibits binding (Ki = 0.25 μM) of the selective cannabinoid receptor subtype 1 (CB1) ligand, [3H]SR141716A, to rat brain membrane. AA-DA also inhibits the anandamide membrane transporter in BL-2H3 basophilic leukemia and C6 glioma cells. AA-DA has at least a 40 fold greater selectivity for CB1 than CB2 receptors in rat brain membranes and has been shown to be more potent than anandamide as a CB1 agonist in undifferentiated N18TG2 neuroblastoma cells. AA-DA induces hypothermia and immobility, and decreases spontaneous activity and pain perception in mice and rats, which supports its action as a CB1 agonist in vivo. AA-DA has been shown to inhibit (IC50 = 0.25 μM) proliferation of human breast MCF-7 cancer cells.
A231 Arachidonyl trifluoromethyl ketone oil, ≥97% (NMR) Inhibits anandamide hydrolysis in vitro; inhibits phospholipase A2.
A9719 Arachidonyl-2′-chloroethylamide hydrate ≥97% (HPLC), oil Potent and selective neuronal CB1 cannabinoid receptor agonist.
A0580 Arachidonylethanolamide ≥97.0% (TLC), oil An arachidonic acid derivative that is an endogenous ligand for the CB cannabinoid receptor and for the VR1 vanilloid receptor. Inhibits calcium currents in neuroblastomas and neurons. Activates the MAP kinase signaling pathway. Inhibits proliferation and induces apoptosis of lymphocytes and human breast cancer cells.
PZ0205 CE-178253 benzenesulfonate salt ≥98% (HPLC) CE-178253 is an extremely potent and selective CB1 antagonist with sub-nanomolar potency. In binding assays, CE-178253 has a 0.33 nM Ki for human CB1, vs. a Ki of > 10 mM for human CB2.
SML0805   CID16020046 ≥98% (HPLC) CID16020046 is a potent and a selective GPR55 antagonist that inhibits GPR55-mediated ERK1/2 phosphorylation. CID16020046 inhibits LPI-induced Ca2+ signaling in HEK-GPR55 cells.
C1112 CP-55940 >98% (HPLC), powder CP-55940 is a selective cannabinoid receptor agonist.
PZ0019   CP-945,598 ≥98% (HPLC) CP-945,598 is a potent, selective, high affinity and competitive cannabinoid type 1 (CB1) receptor antagonist. CP-945,598 inhibits both basal and cannabinoid agonist-mediated CB1 receptor signaling in vitro and in vivo. CP-945,598 exhibits anorectic activity in two models of acute food intake in rodents, fast-induced re-feeding and spontaneous, nocturnal feeding.
C6888 Cannabinol analytical standard Major metabolite of tetrahydrocannabinol that is not psychoactive, CB2 cannabinoid receptor agonist with immunosuppressive properties.
SML0563   Docosahexaenoyl ethanolamide ≥98% (HPLC), ethanol solution (5 mg/ml) Docosahexaenoyl ethanolamide (DHEA) is a lipid signaling molecule present in brain and retina at concentrations, similar to those for arachidonoyl ethanolamide. DHEA binds to the rat brain CB1 receptor with a Ki of 324 nM. It exhibits anti-inflammatory and organ protective activity. Studies show that docosahexaenoyl ethanolamide is the mediator of neurite growth and synaptogenesis in hippocampal neurons, resulting in enhanced synaptic activity.
SML0384 Eicosapentaenoyl ethanolamide 5 mg/mL in absolute ethanol, ≥98% (HPLC) Eicosapentaenoyl ethanolamide (EPEA) is a lipid mediator that has been found to suppress lifespan extension resulting from dietary restriction in C. elegans and also to have antiproliferative and anti-inflammatory actions. In C. elegans, it is believed to act as a metabolic signal that couples nutrient availability with growth and lifespan. EPEA is a member of the N-acylethanolamines (NAEs), lipid-derived signaling molecules that include the mammalian endocannabinoid arachidonoyl ethanolamide (AEA). In mammals, NAEs are believed to act primarily through cannabinoid receptors, although they can also interact with a variety of other targets, and EPEA has been shown to act as a CB1 and CB2 receptor agonist. However, C. elegans does not possess clear orthologues of the mammalian cannabinoid receptors which suggests that there are unidentified NAE receptors in nematodes that are possibly conserved mediators of NAE signaling.
SML1926 GAT211 ≥98% (HPLC) New GAT211 is a positive allosteric modulator (PAM) of cannabinoid CB1 receptor signaling. GAT211 was found to amplify the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. GAT211 caused a CB1-dependent suppression of paclitaxel-induced mechanical and cold allodynia with no sign of tolerance over 19 days of administration.
SML0262 GSK575594A ≥98% (HPLC) GSK575594A is a selective agonist of human GPR55. It is specific for human over rodent GPR55. GSK575594A had no activity across a set of more than 200 validated molecular target assays from diverse classes including kinases, proteases and other enzymes, GPCRs, ion channels, nuclear receptors, and membrane transporters.
G1421 GW405833 hydrochloride ≥98% (HPLC), solid GW405833 is a selective cannabanoid CB2 receptor agonist; analgesic. GW405833 binds with high affinity at both human and rat CB2 receptors (Ki′s 3.9 and 3.6 nM); acts as a partial agonist (50% inhibition of forskolin-stimulated cAMP formation compared to full agonist CP55,940). GW405833 has potent analgesic activity in rat models of inflammatory, neuropathic and incisional pain; devoid of CNS effects common with CB1 agonists.
G8173 GW833972A ≥98% (HPLC), powder GW833972A is a CB2 cannabinoid receptor agonist with 1000-fold selectivity relative to CB1. It is, however, 15-fold less potent than HU210 for CB2 (Ki 7.8 vs. 0.52 nM). The antitumor compound oxaliplatin induces marked hypersensitivity to cold, heat, and chemical pain stimuli (to the point where oxaliplatin therapy has to be discontinued). The hyperalgesia effect is almost completely blocked by pretreatment with GW833972A.
GW833972A is a CB2 receptor agonist with 1000-fold selectivity relative to CB1. GW833972A is 15 fold less potent than HU210 for CB2 (Ki 7.8 vs. 0.52 nM). The compound was used to determine the role of CB2 in airway sensory nerve function.
H7909 HU-210 solid (air sensitive) Cannabinoid receptor agonist.
H3042 Hemopressin trifluoroacetate salt ≥98% (HPLC), powder Hemopressin is an endogenous hypotensive nonapeptide derived from hemoglobin. Hemopressin reduces appetite, acting as a cannabinoid CB1 inverse agonist. It blocks signaling by CB(1) receptors but not by other members of family A G protein-coupled receptors (including the closely related CB(2) receptors.
I151 Indomethacin morpholinylamide solid CB2 cannabinoid receptor agonist.
SML1830 JJKK-048 ≥98% (HPLC) JJKK-048 is a cell penetrant ultrapotent and highly selective inhibitor of monoacylglycerol lipase (MAGL) that exhibits a low cross-reactivity with other endocannabinoid targets. JJKK-048 is an irreversible inhibitor that binds to the active site S122.
SML0990 JW651 ≥98% (HPLC) JW651 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). JW651 inhibited mouse MAGL with an IC50 ~38 nM compared to 10,380 for ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG and >100,000 for FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). JW651 was used as the MAGL inhibitor along with JW912, a fluorescent inihibitor of both MAGL and ABHD6.
J4252 JWH-015 ≥98% (HPLC), powder JWH-015 is a selective CB2 cannabinoid receptor agonist.
J3455 JZL 184 hydrate ≥97% (HPLC) JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.
SML0257 JZL195 ≥98% (HPLC) JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and 4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis and elevate 2-AG and AEA levels in vivo.
SML1364 KT109 ≥98% (HPLC) KT109 is a potent and selective inhibitor of Diacylglycerol lipase DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT109 is a potent and selective DAGLβ inhibitor with an IC50 of 42 nM, ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling. KT109 shows some inhibitory activity against PLA2G7 (IC50 = 1 μM) but no inhibitory activity against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 = 16 nM) can be controlled for by use of the related compound, KT195, a potent (IC50 = 10 nM) and selective ABHD6 inhibitor with negligible activity against DAGLβ. KT109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
SML1248 KT182 ≥98% (HPLC) KT182 is a very potent, orally bioavailable, selective inhibitor of ABHD6 (a/b-Hydrolase Domain Containing 6). IC50 = 1.7 nM. KT182 inhibits ABHD6 activity in the brain and liverin mice (ip administration).
SML1249   KT185 ≥98% (HPLC) KT185 is a very potent, selective inhibitor of a/b-Hydrolase Domain Containing 6 (ABHD6). The compond KT185 is orally bioavailable and inhibits ABHD6 activity in the brain and liver of mice.
SML1308   KT195 ≥98% (HPLC) KT195 is a potent (IC50 = 10 nM) and selective inhibitor of α/β-hydrolase domain-containing 6 (ABHD6), a serine hydrolase that acts as an alternative hydrolase of the endocannabinoid 2-arachidonoylglycerol (2-AG). KT195 has negligible activity against other serine hydrolases such as DAGLβ and has been used as a control probe for studies of DAGLβ as well as being a probe on its own to study ABHD6. KT195 treatment of Neuro2A cells caused significant accumulation of 2-AG. KT195 also lowered interleukin-1β (IL-1β) secretion from lipopolysaccharide-treated macrophages suggesting ABHD6 involvement in this activity as well.
SML1250 KT203 ≥98% (HPLC) KT203 is a very potent, selective inhibitor of ABHD6 (IC50 = 0.82 nM). KT203 inhibits ABHD6 activity in the liver, but not the brain following ip injection in mice.
L1164 Linoleyl ethanolamide ≥98%, ethanol solution A structural analogue of the endogenous cannabinoid receptor ligand anandamide.
SML0872 MJN110 ≥98% (HPLC) MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.
SML1340 ML193 trifluoroacetate ≥98% (HPLC) ML193 is a potent and selective piperadinyloxadiazolone antagonist for G protein-coupled receptor (GPCR) GPR55, a receptor for L-α-lysophosphatidylinosi
H1911 N-(4-Hydroxyphenyl)-arachidonylamide ≥98%, ethanol solution  
A2984 N-Arachidonylmaleimide ≥98% (HPLC) N-Arachidonylmaleidmide (NAM) is structurally similar to the MAGL substrate 2-AG and displays a high potency for inhibition of MAGL. It is thought that NAM binds MAGL at the substrate binding site and inhibits enzyme activity through the Michael addition reaction at the Cys201, and to a lesser extent Cys242, residue of MAGL. In cerebellar rat membranes, NAM inhibits MAGL-like activity with an IC50 of 140 nM.
N7912 NESS 0327 ≥98% (HPLC) Potent cannabinoid CB1 receptor antagonist (Ki= 350 fM) with more than 60,000-fold selectivity for the CB1 receptor. Antagonizes the nociceptive effects produced by WIN 55,212-2 in both tail-flick and hot-plate tests. Useful as a tool to study the involvement of CB1 receptor in psychosis, food intake and cognitive impairment.
N8162 NIDA-41020 ≥97% (HPLC), solid NIDA-41020 is a CB1 cannabinoid receptor antagonist. NIDA-41020 is structurally similar to Rimonabant, which is currently in clinical development. NIDA-41020 is less lipophilic; developed at NIDA as a potential radioligand for CB1 receptors, Ki = 4.1 nM [in comparison AM 251, AM 281, SR 141716 (Rimonabant) have Ki of 0.6, 4.5 and 1.8 nM respectively].
N8161 NS309 ≥98% (HPLC), solid NS309 is a Ca2+-activated IK/SK potassium channel activator.
N3785 Nabilone solid, ≥98% (HPLC) CB1 and CB2 cannabinoid receptor agonist.
SML0473   Noladin ether ≥98% (HPLC) Noladin ether (2-Arachidonyl glycerol ether) is a stable analog of the endogenous cannabanoid 2-Arachidonylglycerol (2-AG) with selectivity for CB1 receptors. Noladin ether is a CB1 agonist. The Ki values for CB1 vs CB2 receptors are 21.2 nM and 3 mM, respectively. Noladin ether induces sedation and has modest antinociceptive activity in vivo, and reduces inter ocular pressure after administration in the eye.
O8014 Org 27569 ≥98% (HPLC) Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It significantly increases the binding of CB1 receptor agonist [3H]-CP 55,940 (pKB = 5.67) and causes a significant decrease in specific binding of CB1 receptor inverse agonist SR141716A (Rimonabant; pKB = 5.95); in the reporter gene assay behaves as insurmountable CP 55,940 antagonist; pKB = 7.57 at CB1 receptors in mouse vas deferens
SML1126 PDP-EA ≥98% (HPLC) 3-N-Pentadecylphenolethanolamide (PDP-EA) is an activator of fatty acid amide hydrolase (FAAH) from plant and mammalian species. PDP-EA appears to enhance FAAH activity by reduction of negative feedback from free ethanoloamine.
PZ0158 PF 3845 hydrate ≥98% (HPLC) PF 3845 is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. The endocannabinoid system is a target for therapeutic pain relief. PF-3845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It high selectivity over other enzymes including FAAH-2. In mouse studies, PF-3845 has been shown to raise brain anandamide levels for up to 24 hr; and in a rat model it produced significant reduction of inflammatory pain..
PZ0184 PF-04457845 ≥98% (HPLC) PF-04457845 is a potent, orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. PF-04457845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It was shown to be both potent and selective against other serine hydrolases. It has an IC50 value of 7.2 nM for human FAAH. The endocannabinoid system is a target for therapeutic pain relief. In a rat model of inflammatory pain, PF-04457845 produced significant reduction of inflammatory pain with efficacy comparable to that of naproxen at 10 mg/kg.
SML0389 PF-514273 ≥98% (HPLC) PF-514273 is a highly selective CB1 antagonist. The Ki for binding to CB1 and CB2 receptors is 1 nM and 10 mM, respectively. PF-514273 inhibits food intake and weight gain in rodents.
SML0298 PSNCBAM-1 ≥98% (HPLC) PSNCBAM-1 is an allosteric, non-competitive antagonist of CB-1. The compound blocks the effects of WIN 55212-2 and CP55940, and reduces food intake and weight gain in rats.
P0359 Palmitoylethanolamide Endogenous CB2 cannabinoid receptor agonist.
M186 R(+)-Methanandamide 5 mg/mL in absolute ethanol, ≥96% (HPLC) R(+)-Methanandamide is metabolically stable congener of anandamide that has higher affinity for the cannabinoid receptor. Of the analogs tested, (R)-methanandamide exhibited the highest affinity for the cannabinoid receptor with a Ki of 20 +/- 1.6 nM, 4-fold lower than that of anandamide (Ki = 78 +/- 2 nM). (R)-methanandamide exhibits high stability to aminopeptidase hydrolysis. Experiments with mice have demonstrated that (R)-methanandamide also posseses cannabimimetric properties in vivo, as established by the four tests of hypothermia, hypokinesia, ring immobility, and antinociception.
SML0800   Rimonabant hydrochloride ≥98% (HPLC) Rimonabant hydrochloride (SR-141716A) is a potent and selective CB1 cannabinoid inverse agonist/antagonist with a Ki of 1.6 nM, minimal affinity for CB2, and and some GPR55 agonist activity. Rimonabant was developed as an anti-obesity drug because of its appetite suppressant activity, but was taken off the market because of side effects of depression and anxiety.
SML1899 SR144528 ≥98% (HPLC) SR144528 is a potent and highly selective cannabinoid CB2 receptor inverse agonist. SR144528 exhibited a Ki of 0.6 nM at CB2 compared to 400 nM at the related CB1 receptor.
SML0514 UCM710 ≥98% (HPLC) UCM710 is a dual inhibitor of fatty acid amide hydrolase (FAAH) and α/β hydrolase domain 6 (ABHD6) the enzymes that hydrolyze endocannabinoids. UCM710 augments both N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) levels in neurons. UCM710 does not inhibit monoacylglycerol lipase (MAGL).
V3264 VDM 11 ≥98% (HPLC), oil Potent, selective anandamide membrane transporter (AMT) inhibitor.
V2389 Virodhamine hydrochloride >90% (GC), oil Endogenous cannabinoid; partial CB1 receptor agonist; full CB2 receptor agonist.
SML1641 WWL70 ≥98% (HPLC) WWL70 is a selective inhibitor of α/β-hydrolase domain-containing 6 (ABHD6), a serine hydrolase that acts as an alternative hydrolase of the endocannabinoid 2-arachidonoylglycerol (2-AG). It has an IC50 value of 55-70 nM and 90-95% inihibition of ABDH6. WWL70 hs been used in a variety of studies as an ABHD6 antagonist. It was shown to rescue impaired function of mGluR5 signaling, resulting in pain inhibition in arthritic rats. WWL70 was also used to show that ABHD6 is involved in brown adipose function and white adipose browning, and is a potential therapeutic target for obesity and type 2 diabetes.
T2386 Δ9-Tetrahydrocannabinol solution ethanol solution Δ9-Tetrahydrocannabinol or Δ9-THC is a psychoactive ingredient in marijuana that is known to function as a neuroprotective antioxidant21. In vivo microdialysis studies have reported that Δ9-THC can enhance extracellular dopamine efflux in the nucleus accumbens of conscious, freely-moving rats22.
Agonist at CB1 and CB2 cannabinoid receptors. Hallucinogen; major psychoactive component of marijuana from Cannabis sativa.