| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
PAR2 ( IC50 = 23 nM )
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| ln Vitro |
AZ3451 is a PAR2 antagonist that affects apoptosis, autophagy, cellular senescence, and the inflammatory response in osteoarthritis (OA). AZ3451 stops cartilage deterioration, IL-1β-induced inflammatory response, and chondrocytes from prematurely senescing. By inducing autophagy, AZ3451 reduces the apoptosis of chondrocytes in vitro. NF-κB, PI3K/AKT/mTOR, and P38/MAPK pathways are all involved in AZ3451's protective effects. [2]
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| ln Vivo |
In a rat osteoarthritis (OA) model, intra-articular injection of AZ3451 can reduce the cartilage degradation caused by surgery.[/2]
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| Cell Assay |
The cartilage tissue of one-week-old Sprague-Dawley rats' knee joints is the source of primary rat chondrocytes. The cartilage pieces undergo sequential digestion using 0.2% trypsin and 0.25% collagenase II dissolved in Dulbecco's Modified Eagle Medium (DMEM) culture medium. The freed chondrocytes are gathered and incubated in DMEM enhanced with 10% FBS, 100 units/ml of penicillin, and 100 μg/ml of streptomycin. The cells are treated with 10 μM AZ3451 in the presence or absence of 10 ng/mL IL-1β up to about 80% confluences. In our experiment, we utilize chondrocytes from passages 1-3 in order to prevent phenotypic loss.
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| Animal Protocol |
male 8-week-old Sprague–Dawley rats
100 μl (50 μg/ml) intra-articular injection |
| References | |
| Additional Infomation |
AZ3451 is a member of the class of benzimidazoles that is 1H-benzimidazole substituted by (1S)-1-cyclohexylethyl, 6-bromo-1,3-benzodioxol-5-yl, and 4-(cyanoanilino)acyl groups at positions 1, 2 and 5, respectively. It is an allosteric modulator of protease-activated receptor 2 (IC50 = 23 nM) and exhibits anti-osteoarthritis properties. It has a role as an anti-inflammatory agent, a PAR2 negative allosteric modulator and an autophagy inducer. It is a secondary carboxamide, a nitrile, a member of benzimidazoles, a member of benzodioxoles and an organobromine compound.
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| Molecular Formula |
C30H27BRN4O3
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|---|---|
| Molecular Weight |
571.464386224747
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| Exact Mass |
570.13
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| Elemental Analysis |
C, 63.05; H, 4.76; Br, 13.98; N, 9.80; O, 8.40
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| CAS # |
2100284-59-9
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| PubChem CID |
126961335
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| Appearance |
White to light brown solid powder
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| LogP |
6.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
38
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| Complexity |
882
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C1CCCCC1)N2C3=C(C=C(C=C3)C(=O)NC4=CC=C(C=C4)C#N)N=C2C5=CC6=C(C=C5Br)OCO6
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| InChi Key |
FJAOGFGHTPYADT-SFHVURJKSA-N
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| InChi Code |
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
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| Chemical Name |
2-(6-bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]benzimidazole-5-carboxamide
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| Synonyms |
AZ-3451; AZ3451; AZ 3451
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~175.0 mM)
Ethanol: ~100 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7499 mL | 8.7495 mL | 17.4990 mL | |
| 5 mM | 0.3500 mL | 1.7499 mL | 3.4998 mL | |
| 10 mM | 0.1750 mL | 0.8750 mL | 1.7499 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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