Cannabinoid Receptor
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
Cannabinoid Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
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| S9413 |
YangoninYangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
||
| S3021 |
RimonabantRimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
||
| S2819 |
AM251AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
Inhibition of CB1 suppresses the proliferation and migration and induces apoptosis of RCC cells. a Western blot analysis of CB1 protein in RCC cell lines (786-O, CAKI-1, CAKI-2, 769-P, A498, and ACHN) and normal cell line HK-2, and β-actin was used as a loading control for western blot assays. b RCC cell lines were treated at the indicated concentrations for different time points, and the cell viability was analyzed by MTT assay. AM251-induced cell death in 769-P cells in a dose- and time-dependent manner. c AM251-induced cell death in 786-O cells in a dose- and timedependent manner. d AM251 reduced migration in 786-O and 769-P cell lines at 20 and 30 μM concentrations. e The transmembrane cell number of 786-O and 769-P cells after treatment with different concentrations of AM251 significantly decreased compared with untreated control. |
|
| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl 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. Phase 1. |
||
| S8694 |
CID16020046 (CID 16020046)CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. |
||
| S6735 |
JD-5037JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. |
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| S1544 |
AM1241AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
AM1241 increased ki67+ positive cells and decreased cardiac fibrosis after MI. A, Masson's trichrome-stained myocardial sections from a sub- group of animals at POD 28. B, Comparison of fibrosis areas in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. C, Immunohistochemistry of Ki67 (green), and DAPI (blue) staining in adjacent infarction areas. D, Comparison of ki67 positive cells in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. Scale bar, 20 μm. |
|
| S2854 |
BML-190BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
|
| S8017New |
WIN 55, 212-2 mesylateWIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. |
||
| S0412New |
Bay 59-3074Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties. |
||
| S2778 |
GW842166XGW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2. |
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| S1534 |
Org 27569Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. |
||
| S9048 |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9413 |
YangoninYangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3021 |
RimonabantRimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
||
| S2819 |
AM251AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
Inhibition of CB1 suppresses the proliferation and migration and induces apoptosis of RCC cells. a Western blot analysis of CB1 protein in RCC cell lines (786-O, CAKI-1, CAKI-2, 769-P, A498, and ACHN) and normal cell line HK-2, and β-actin was used as a loading control for western blot assays. b RCC cell lines were treated at the indicated concentrations for different time points, and the cell viability was analyzed by MTT assay. AM251-induced cell death in 769-P cells in a dose- and time-dependent manner. c AM251-induced cell death in 786-O cells in a dose- and timedependent manner. d AM251 reduced migration in 786-O and 769-P cell lines at 20 and 30 μM concentrations. e The transmembrane cell number of 786-O and 769-P cells after treatment with different concentrations of AM251 significantly decreased compared with untreated control. |
|
| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl 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. Phase 1. |
||
| S8694 |
CID16020046 (CID 16020046)CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. |
||
| S6735 |
JD-5037JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1544 |
AM1241AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
AM1241 increased ki67+ positive cells and decreased cardiac fibrosis after MI. A, Masson's trichrome-stained myocardial sections from a sub- group of animals at POD 28. B, Comparison of fibrosis areas in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. C, Immunohistochemistry of Ki67 (green), and DAPI (blue) staining in adjacent infarction areas. D, Comparison of ki67 positive cells in all groups. *, P<0.05 vs. MI group; #, P<0.05 vs. MI+AM group. Scale bar, 20 μm. |
|
| S2854 |
BML-190BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
|
| S8017New |
WIN 55, 212-2 mesylateWIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. |
||
| S0412New |
Bay 59-3074Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties. |
||
| S2778 |
GW842166XGW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2. |
||
| S1534 |
Org 27569Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9048 |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
