WOBE437 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 2.5 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 1 mg/ml

form 

A crystalline solid

color 

white to beige

WOBE437 Usage And Synthesis

Description

WOBE437 is a potent endocannabinoid uptake inhibitor with IC₅₀ values of 10 and 283 nM for arachidonoyl ethanolamide (AEA; ) and 2-arachidonoyl glycerol (2-AG; ) uptake, respectively, in U937 cells. It is greater than 1,000-fold selective for endocannabinoid transporters over fatty acid amide hydrolase (FAAH; ) and the 2-AG hydrolyzing enzymes MAGL, ABHD6, and ABHD12. WOBE437 inhibits AEA uptake in FAAH-deficient HMC-1 human mast cells and Neuro2a mouse neuroblastoma cells (IC₅₀s = 137 and 55 nM, respectively) and reduces AEA uptake by 50% in rat cortical neurons when used at a concentration of 1 μM. It also reduces 2-AG uptake by 40% in Neuro2a cells at a concentration of 5 μM. In vivo, WOBE437 increases AEA and 2-AG levels by 1.5-fold in mouse brain but not peripheral tissues after intraperitoneal administration of a 10 mg/kg dose for seven days. WOBE437 (10 mg/kg) also induces a typical tetrad of hypothermia, catalepsy, analgesia, and hypomotility in mice, indicating it also acts as an indirect cannabinoid (CB) receptor 1 agonist.

Uses

WOBE437 is a biochemical reagent.

References

[1] ANDREA CHICCA. Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2017, 114 25: E5006-E5015. DOI: 10.1073/pnas.1704065114