SR-144528

SKU: orb1706606

Description

SR144528 is a potent and selective CB2 receptor antagonist (Ki = 0.6 nM) that also inhibits microsomal ACAT activity (IC50 = 3.6 µM). This dual activity makes it a valuable research tool for investigating cannabinoid system pharmacology and cholesterol metabolism in both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 192703-06-3
• MW: 476.07
• Purity: >98%
• Formula: C₂₉H₃₄ClN₃O
• SMILES: [H][C@@]12CC[C@@](C)(C1)[C@H](NC(=O)c1cc(-c3ccc(Cl)c(C)c3)n(Cc3ccc(C)cc3)n1)C2(C)C
• Target: GPCR
• Solubility: Soluble in DMSO (up to 20 mg/ml, with warming).

Bioactivity

• Target IC50:
  CB2 receptor:0.6 nM(ki)
• In Vivo:
  SR144528 enhances delayedgastric emptying.
• 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. In Raw 264.7 macrophages, SR144528 reduces the activity of caspase 3. SR144528(10 μM) inhibits microsomal ACAT activity(68%).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SR 144528, SR144528, SR-144528, CannabinoidReceptor, Cannabinoid Receptor, CB2 receptor, CB2

Compound Identifiers

PubChem CID

3081355