WOBE437
WOBE437 Basic information
- Product Name:
- WOBE437
- Synonyms:
-
- WOBE437
- 2,4-Dodecadienamide, N-[2-(3,4-dimethoxyphenyl)ethyl]-, (2E,4E)-
- (2E,4E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-2,4-dodecadienamide
- CAS:
- 2108100-73-6
- MF:
- C22H33NO3
- MW:
- 359.5
- Mol File:
- 2108100-73-6.mol
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
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.