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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 Chemical Structure
SR144528, CAS 192703-06-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 36.00
5 mg In stock $ 87.00
10 mg In stock $ 157.00
25 mg In stock $ 357.00
50 mg In stock $ 533.00
100 mg In stock $ 769.00
1 mL * 10 mM (in DMSO) In stock $ 96.00
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Purity: 99.6%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 1 year

Solubility Information

DMSO: 45.0 mg/mL (94.5 mM), Sonication is recommended.

TargetMolReferences 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.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Bioactive Compound Library

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Keywords

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

 

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