An allosteric agonist of CB1; the R-(+)-enantiomer of GAT229 and GAT211; increases β-arrestin recruitment

GAT228 – 10 mg

Brand:
Cayman
CAS:
1446648-15-2
Storage:
-20
UN-No:
Non-Hazardous - /

GAT228 is an allosteric agonist of cannabinoid receptor 1 (CB1), the R-(+)-enantiomer of the CB1 positive allosteric modulator (PAM) GAT229 (Item No. 24486), and a component of the racemic mixture GAT211, which acts as both an agonist and PAM.{35179,48089} GAT228 increases β-arrestin recruitment, cAMP inhibition, and ERK1/2 and PLCβ3 phosphorylation in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner.{35179} Unlike GAT229, GAT228 has no effect on the binding of the CB receptor agonist CP 55,940 to membranes from CHO cells expressing hCB1 when used at concentrations up to 1 µM. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.{48089}  

 

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SKU: 24485 - 10 mg Category:

Description

An allosteric agonist of CB1; the R-(+)-enantiomer of GAT229 and GAT211; increases β-arrestin recruitment, cAMP inhibition, and ERK1/2 and PLCβ3 phosphorylation in HEK293A cells expressing hCB1-GFP in a concentration-dependent manner; has no effect on the binding of CP 55,940 to membranes from CHO cells expressing hCB1 at up to 1 µM; inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons at 1 µM

Formal name: 3-[(1R)-2-nitro-1-phenylethyl]-2-phenyl-1H-indole

Synonyms: 

Molecular weight: 342.4

CAS: 1446648-15-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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