AZ-3451 |
| Catalog No.GC18152 |
AZ-3451 est un puissant antagoniste du récepteur 2 activé par la protéase (PAR2) avec une IC50 de 23 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2100284-59-9
Sample solution is provided at 25 µL, 10mM.
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AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.
AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocket within the membrane. The interaction of AZ3451 with PAR2 is predominately hydrophobic in nature. AZ3451 binds to a remote allosteric site outside the helical bundle, which prevents structural rearrangements required for receptor activation and signaling.
IC50/KD
| IP-One(SLIGRL) | 23±1nM(n=72) |
| FLIPR(SLIGRL) | 5.4±1.1nM(n=11) |
| FLIPR(Trypsin) | 6.6±1.1μM(n=9) |
| Biacore(KD) | 13.5±3nM(n=3) |
| β-arrestin-2(PAR1) | >50μM(n=1) |
| β-arrestin-2(PAR2) | <2.5nM(n=1) |
| β-arrestin-2(PAR4) | 0.38μM(n=1) |
References:
1. Cheng RKY, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.
| Cas No. | 2100284-59-9 | SDF | |
| Chemical Name | (S)-2-(6-bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1H-benzo[d]imidazole-5-carboxamide | ||
| Canonical SMILES | BrC1=CC2=C(OCO2)C=C1C3=NC4=CC(C(NC5=CC=C(C#N)C=C5)=O)=CC=C4N3[C@@H](C)C6CCCCC6 | ||
| Formula | C30H27BrN4O3 | M.Wt | 571.46 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7499 mL | 8.7495 mL | 17.499 mL |
| 5 mM | 0.35 mL | 1.7499 mL | 3.4998 mL |
| 10 mM | 0.175 mL | 0.875 mL | 1.7499 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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