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.

AM841 is a cannabinoid superagonist and a covalent, irreversible full agonist of CB1. AM841 can activate peripheral CB1 receptors to reduce excitatory neurotransmission and GI smooth muscle contractility, and inhibit synaptic transmission. AM841 is peripherally restricted at low doses in mice, with extremely low brain penetration, potently inhibits gastrointestinal motility, and can reverse acute stress-induced hyperaccelerated gastrointestinal transit; at high doses, it can produce the classic tetrad of central cannabinoid phenotypes (analgesia, catalepsy, hypothermia, decreased spontaneous activity). AM841 can improve intestinal inflammation in mouse colitis models. AM841 induces transient stress-induced hyperthermia. AM841 can be used for research on gastrointestinal motility disorders and colitis.

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.