BR103
Based on 1 Customer Validation
BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding.
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- Pureté: 99.66%
- CAS No.: 1434873-26-3
- Formule: C24H28N6O3
- Masse moléculaire:448.52
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
Activité biologique
C3aR[1]
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
BR103 can be used in animal modeling to create inflammatory paw edema models in Wistar rats. BR103 remains structurally intact and undegraded after in vitro exposure to rat plasma and rat liver microsomes, which are rich in cytochrome P450 enzymes. This in vitro stability of BR103 suggests potentially low in vivo clearance, high stability, and bioavailability. Paw edema induced by subplantar injection of BR103 peaks at 0.5 hours and resolves by 24 hours[2][3].
Administration: 350 ng • Intraplantar (i.pl.) injection • single dose
Histological changes: Localized paw edema; infiltration of macrophages and neutrophils at the inflammation site.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1434873-26-3
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Appearance Solid
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Masse moléculaire 448.52
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Formule C24H28N6O3
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Color White to off-white
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SMILES
N=C(N)NCCC[C@@H](C(O)=O)NC(C1=C(C)N=C(C(C2=CC=CC=C2)C3=CC=CC=C3)N1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
DMSO : 100 mg/mL (222.96 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 (stored under nitrogen). 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 (stored under nitrogen). 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: ≥ 2.5 mg/mL (5.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dantas de Araujo A, et al. Europium-Labeled Synthetic C3a Protein as a Novel Fluorescent Probe for Human Complement C3a Receptor. Bioconjug Chem. 2017 Jun 21;28(6):1669-1676. [Content Brief]
[2]. Lohman RJ, et al. Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Nat Commun. 2017 Aug 24;8(1):351. [Content Brief]
[3]. Rowley JA, et al. Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. J Med Chem. 2020 Jan 23;63(2):529-541. [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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2296 mL | 11.1478 mL | 22.2956 mL | 55.7389 mL |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4591 mL | 11.1478 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL | 5.5739 mL | |
| 15 mM | 0.1486 mL | 0.7432 mL | 1.4864 mL | 3.7159 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1148 mL | 2.7869 mL | |
| 25 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2296 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8580 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3935 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 80 mM | 0.0279 mL | 0.1393 mL | 0.2787 mL | 0.6967 mL | |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5574 mL |
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