A CB2 receptor agonist; selective for CB2 over CB1 (Kis = 7.1 and 580 nM); considered a protean agonist because it has neutral antagonist and partial agonist activity

AM1241 – 1 mg

Brand:
Cayman
CAS:
444912-48-5
Storage:
-20
UN-No:
Non-Hazardous - /

AM1241 is a cannabinoid (CB) receptor agonist that is selective for CB2 over CB1 with Ki values of 7.1 and 580 nM for human recombinant receptors transfected into HEK and CHO cells, respectively, in a radioligand binding assay.{14812,14986} It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized.{14812} It is also acts in a species-dependent manner in vitro, acting as an agonist at human CB2 receptors (EC50 = 190 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 216 and 463 nM, respectively).{18107} AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB2 receptor-selective antagonist AM630 (Item No. 10006974) but not by the CB1 receptor-selective antagonist AM251 (Item No. 71670). AM1241 is neuroprotective, preventing HIV-1 glycoprotein Gp120-induced apoptosis in primary human and murine neural progenitor cells and increasing cell survival and differentiation. It increases hippocampal neurogenesis and decreases astro- and gliogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days.{38336} AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).{38337}  

 

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SKU: 10010118 - 1 mg Category:

Description

A CB2 receptor agonist; selective for CB2 over CB1 (Kis = 7.1 and 580 nM); considered a protean agonist because it has neutral antagonist and partial agonist activity, depending on the assay utilized; acts in a species-dependent manner in vitro, acting as an agonist at human CB2 receptors (EC50 = 190 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 216 and 463 nM, respectively); produces antinociception to thermal stimuli in rat hindpaw; neuroprotective, preventing Gp120-induced apoptosis in vitro and increasing survival and differentiation of neural progenitor cells; increases hippocampal neurogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days; delays motor impairment in a murine model of ALS

Formal name: (2-iodo-5-nitrophenyl)-(1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl)methanone

Synonyms: 

Molecular weight: 503.3

CAS: 444912-48-5

Purity: ≥97%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Neurodegenerative Disorders||Research Area|Neuroscience|Neuroprotection||Research Area|Neuroscience|Pain Research

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