AZ3451

Catalog No.S9744 Batch:S974401

Technical Data

Formula	C₃₀H₂₇BrN₄O₃
Molecular Weight	571.46	CAS No.	2100284-59-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (174.99 mM)
		Ethanol	100 mg/mL (174.99 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

PAR2 ^[1]
(Cell-free assay)

23 nM

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.^[2]

In vivo

Intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines chondrocytes Concentrations 10 μM Incubation Time 48 h Method Primary rat chondrocytes are derived from the knee joint cartilage tissue of 1-week-old Sprague–Dawley rats. Cartilage pieces are sequential digested with 0.2% trypsin and 0.25% collagenase II dissolved in Dulbecco’s Modified Eagle Medium (DMEM) culture medium. The released chondrocytes are collected and cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin and 100 μg/ml streptomycin. Up to approximately 80% confluences, cells are treated with 10 μM AZ3451 in the presence or absence of 10 ng/mL IL-1β. Passages 1–3 chondrocytes are used in our experiment to avoid the phenotype loss.
Animal Study:^{^[2]}	Animal Models male 8-week-old Sprague–Dawley rats Dosages 100 μl (50 μg/ml) Administration intra-articular injection

Cell Assay:^{^[2]}

Cell lines
chondrocytes
Concentrations
10 μM
Incubation Time
48 h
Method
Primary rat chondrocytes are derived from the knee joint cartilage tissue of 1-week-old Sprague–Dawley rats. Cartilage pieces are sequential digested with 0.2% trypsin and 0.25% collagenase II dissolved in Dulbecco’s Modified Eagle Medium (DMEM) culture medium. The released chondrocytes are collected and cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin and 100 μg/ml streptomycin. Up to approximately 80% confluences, cells are treated with 10 μM AZ3451 in the presence or absence of 10 ng/mL IL-1β. Passages 1–3 chondrocytes are used in our experiment to avoid the phenotype loss.

Animal Study:^{^[2]}

Animal Models
male 8-week-old Sprague–Dawley rats
Dosages
100 μl (50 μg/ml)
Administration
intra-articular injection

References

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SHIPPING AND STORAGE
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