AZ3451

SKU: orb1296273

Description

AZ3451 is a potent allosteric antagonist of protease-activated receptor 2 (PAR2), exhibiting an IC50 of 23 nM. This small molecule is a valuable research tool for investigating PAR2-mediated signaling in inflammation, pain, and cancer within in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2100284-59-9
• MW: 571.46
• Purity: 98.44% (May vary between batches)
• Formula: C₃₀H₂₇BrN₄O₃
• SMILES: C[C@@H](C1CCCCC1)n1c(nc2cc(ccc12)C(=O)Nc1ccc(cc1)C#N)-c1cc2OCOc2cc1Br
• Target: Protease-activated Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.77 mM);H2O:Insoluble;DMSO:80 mg/mL (139.99 mM)

Bioactivity

• Target IC50:
  PAR2:23 nM（kd）
• In Vitro:
  AZ3451 is selective for PAR2 over PAR4 and PAR1 (IC50s = <2.5, 380, and >50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 μM.
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Storage & Handling

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

Alternative Names

Thrombin receptors, Proteaseactivated Receptor, Protease Activated Receptor (PAR), Protease-Activated Receptor (PAR), ProteaseactivatedReceptor, AZ 3451, AZ3451, AZ-3451, inhibit, PAR-2, Inhibitor

Compound Identifiers

PubChem CID

126961335