AZ8838
Based on 1 Customer Validation
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
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- Pureté: 99.30%
- CAS No.: 2100285-41-2
- Formule: C13H15FN2O
- Masse moléculaire:234.27
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PAR2 |
AZ8838 binds in an occluded pocket[1].
AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70 ± 0.02[1].
AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84 ± 0.02)[1].
AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) and β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats, PAR2 agonist 2f-LIGRLO-NH2 induced acute oedema model[1]
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Dosage:10 mg/kg
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Administration:Oral administration, once, 2 h prior
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Result:Showed 60% reduction of paw swelling. Inhibited 2f-LIGRLO-NH2 induced activated mast cells, inhibited 2f-LIGRLO-NH2 decreased tryptase-positive (AA1+ve) intact mast cells in paw, blocked histamine release.
Chemical Information
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CAS No. 2100285-41-2
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Appearance Solid
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Masse moléculaire 234.27
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Formule C13H15FN2O
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Color Off-white to light yellow
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SMILES
O[C@H](C1=NC=CN1)C2=C(C=C(C=C2)F)CCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 200 mg/mL (853.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (21.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (21.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kennedy AJ, et al. Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition. Commun Biol. 2020 Dec 17;3(1):782. [Content Brief]
[2]. Cheng RKY, Fiez-Vandal C, Schlenker O, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017;545(7652):112-115. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.2686 mL | 21.3429 mL | 42.6858 mL | 106.7145 mL |
| 5 mM | 0.8537 mL | 4.2686 mL | 8.5372 mL | 21.3429 mL | |
| 10 mM | 0.4269 mL | 2.1343 mL | 4.2686 mL | 10.6714 mL | |
| 15 mM | 0.2846 mL | 1.4229 mL | 2.8457 mL | 7.1143 mL | |
| 20 mM | 0.2134 mL | 1.0671 mL | 2.1343 mL | 5.3357 mL | |
| 25 mM | 0.1707 mL | 0.8537 mL | 1.7074 mL | 4.2686 mL | |
| 30 mM | 0.1423 mL | 0.7114 mL | 1.4229 mL | 3.5571 mL | |
| 40 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6679 mL | |
| 50 mM | 0.0854 mL | 0.4269 mL | 0.8537 mL | 2.1343 mL | |
| 60 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7786 mL | |
| 80 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3339 mL | |
| 100 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0671 mL |
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