Cannabinoid Receptor Agonist

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.

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 K_i values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC₅₀ and EC₅₀ is 0.8 μM and 0.12 μM, respectively.

MK-5596 is an efficient, selective and orally active CB1R (IC₅₀ = 1.0 nM, EC₅₀ = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC₅₀ = 3.3 μM, CYP2C8: IC₅₀ = 11 μM, CYP2C9: IC₅₀ = 18 μM, CYP2D6: IC₅₀ = 6 μM). MK-5596 can be used for research on conditions such as obesity.

AM12814 is a potent and partial CB1 and CB2 agonist with K_i values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.

CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with K_is 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.

2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with K_i values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity.

(E)-RNB-61 is the E configuration of RNB-61 (HY-163825). RNB-61 is an orally active cannabinoid CB2 receptor (CB2R) agonist with a K_i range of 0.13 nM to 1.81 nM. RNB-61 has renal protective and/or anti-fibrotic effects.

Δ9-THCB (Δ9-Tetrahydrocannabutol) has a high affinity for human CB1 and CB2 receptors with the K_i values of 15 nM and 51 nM, respectively. Δ9-THCB (Δ9-Tetrahydrocannabutol) has analgesic and anti-inflammatory activities and plays partial agonistic effects on CB1 receptor in mice.

Mead ethanolamide is an endogenous cannabinoid receptor agonist with K_d values of 753 nM and 1810 nM against CB1 and CB2, respectively.

Levonantradol (l-Nantradol) hydrochloride is an analog of delta (9)-tetrahydrocannabinol. Levonantradol acting as a potent anti-analgesic agent.

PM226 is a selective cannabinoid CB2R agonist (K_i (CB2R)=13 nM; EC₅₀ (CB2R)=39 nM; K_i (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.

AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 K_i of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity.

RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2.