AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM.

Product information

CAS Number: 2100284-59-9

Molecular Weight: 571.46

Formula: C30H27BrN4O3

Chemical Name: (S)-2-(6-Bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1Hbenzo[d]imidazole-5-carboxamide

Smiles: C[C@@H](C1CCCCC1)N1C(=NC2=CC(=CC=C12)C(=O)NC1=CC=C(C=C1)C#N)C1=CC2OCOC=2C=C1Br

InChiKey: FJAOGFGHTPYADT-SFHVURJKSA-N

InChi: InChI=1S/C30H27BrN4O3/c1-18(20-5-3-2-4-6-20)35-26-12-9-21(30(36)33-22-10-7-19(16-32)8-11-22)13-25(26)34-29(35)23-14-27-28(15-24(23)31)38-17-37-27/h7-15,18,20H,2-6,17H2,1H3,(H,33,36)/t18-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(174.99 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AZ3451 is a PAR2 antagonist that plays a part in inflammation response, apoptosis, autophagy and cellular senescence during Osteoarthritis (OA). AZ3451 prevents the IL-1β-induced inflammation response, cartilage degradation and premature senescence in chondrocytes. AZ3451 attenuates chondrocytes apoptosis by activating autophagy in vitro. The P38/MAPK, NF-κB and PI3K/AKT/mTOR pathways are involved in the protective effect of AZ3451.

In Vivo:

Intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.

References:

1. Xiaojian Huang, et al. Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.
2. Robert K Y Cheng, et al. Nature. 2017 May 4;545(7652):112-115.

Products are for research use only. Not for human use.