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SR144528

Catalog No. T16928 CAS 192703-06-3

SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).

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SR144528, CAS 192703-06-3

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Purity: 98%

Biological Description

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Description	SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).
Targets&IC50	CB2 receptor:0.6 nM(ki)
In vitro	SR144528(1 μM) stimulates the forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells in a concentration-dependent manner with an EC50 of 26 nM[1]. In Raw 264.7 macrophages, SR144528 reduces the activity of caspase 3. SR144528(10 μM) inhibits microsomal ACAT activity(68%)[2].
In vivo	SR144528 enhances delayedgastric emptying[3].

Molecular Weight	476.05
Formula	C29H34ClN3O
CAS No.	192703-06-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45.0 mg/mL (94.5 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Rinaldi-Carmona M, et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther. 1998 Feb;284(2):644-50. 2. Thewke D, et al. AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors. Biochem Biophys Res Commun. 2009 Apr 3;381(2):181-6. 3. Abalo R, et al. The cannabinoid antagonist SR144528 enhances the acute effect of WIN 55,212-2 on gastrointestinal motility in the rat. Neurogastroenterol Motil. 2010 Jun;22(6):694-e206.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SR144528 192703-06-3 GPCR/G Protein Cannabinoid Receptor SR-144528 Inhibitor inhibitor inhibit

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