GW-405833

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin. GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF)[2][3][4][5].

180002-83-9

L768242

12352005

H301, H413

Cannabinoid Receptor; Endogenous Metabolite; HIF/HIF Prolyl-Hydroxylase; Interleukin Related; TNF Receptor

Reference compound

Apoptosis; GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling

COVID-19-immunoregulation

Inflammation/Immunology; Neurological Disease

https://www.medchemexpress.com/gw-405833.html

10mM

98.91

DMSO : 116.67 mg/mL (ultrasonic; warming; heat to 60°C)

O=C(C1=C(C(Cl)=CC=C1)Cl)N2C3=C(C=C(OC)C=C3)C(CCN4CCOCC4)=C2C

C23H24Cl2N2O3

447.35

H301, H413

[1]Li AL, et al. Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther. 2017 Aug;362 (2) :296-305.|[2]Li J, et al. Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation. Medchemcomm. 2019 Sep 17;10 (11) :1935-1947. |[3]Parlar A, Arslan SO, Doğan MF, et al. The exogenous administration of CB2 specific agonist, GW405833, inhibits inflammation by reducing cytokine production and oxidative stress. Exp Ther Med. 2018;16 (6) :4900-4908.|[4]Marini P, Cascio MG, King A, Pertwee RG, Ross RA. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol. 2013;169 (4) :887-899. |[5]Cai SL, et al. CB2R agonist GW405833 alleviates acute liver failure in mice via inhibiting HIF-1α-mediated reprogramming of glycometabolism and macrophage proliferation. Acta Pharmacol Sin. 2023 Jul;44 (7) :1391-1403.|[6]Valenzano KJ, et al. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48 (5) :658-72.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1

No Development Reported