A potent endocannabinoid uptake inhibitor (IC50s = 10 and 283 nM for AEA and 2-AG

WOBE437 – 1 mg

Brand:
Cayman
CAS:
2108100-73-6
Storage:
-20
UN-No:
Non-Hazardous - /

WOBE437 is a potent endocannabinoid uptake inhibitor with IC50 values of 10 and 283 nM for arachidonoyl ethanolamide (AEA; Item No. 90050) and 2-arachidonoyl glycerol (2-AG; Item No. 62160) uptake, respectively, in U937 cells.{40064} It is greater than 1,000-fold selective for endocannabinoid transporters over fatty acid amide hydrolase (FAAH; Item No. 10010183) 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.  

 

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Description

A potent endocannabinoid uptake inhibitor (IC50s = 10 and 283 nM for AEA and 2-AG, respectively, in U937 cells); inhibits AEA uptake in FAAH-deficient HMC-1 human mast cells and Neuro2a mouse neuroblastoma cells (IC50s = 137 and 55 nM, respectively); increases AEA and 2-AG levels by 1.5-fold in mouse brain but not peripheral tissues (10 mg/kg, i.p. for seven days); induces a typical tetrad of hypothermia, catalepsy, analgesia, and hypomotility in mice

Formal name: (2E,4E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-2,4-dodecadienamide

Synonyms: 

Molecular weight: 359.5

CAS: 2108100-73-6

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids||Research Area|Neuroscience|Pain Research

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