BER-5
Based on 1 Customer Validation
BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP) (HY-P0201)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 724709-67-5
- Formule: C20H16O4
- Masse moléculaire:320.34
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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
BER-5 (12.5-50 μM) inhibits SP-induced degranulation of LAD2 cells specifically manifested by the suppression of β-hexosaminidase (30 min), histamine (2 h), and IL-8 release (6 h)[1].
BER-5 (0-100 μM ,30 min) (IC50 = 20.64 μM) inhibit the SP-induced release of β-hexosaminidase more effectively in LAD2 cells compared with Bergaptol (BER; HY-76316) (IC50 = 46.79 μM) and Imperatorin (IMP; HY-N0285) (IC50 = 99.73 μM)[1].
BER-5 (50 μM) slightly increased the half-maximal effective concentration (EC50) while significantly decreasing the maximum efficiency (Emax) response of SP in LAD2 cells[1].
BER-5 (12.5-50 μM) inhibits degranulation induced by C48/80 (HY-130592), (R)-ZINC-3573 (HY-118069), Rocuronium Bromide (HY-17440) and Ciprofloxacin (HY-B0356) in LAD2 cells, suggesting that BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists[1].
BER-5 (12.5-50 μM, 30 min) inhibits Ca2+ mobilization induced by SP in a concentration-dependent manner in MrgX2-HEK293 cells[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:6-8 weeks adult male C57BL/6 mice treated SP (10 μM)
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Dosage:6.25, 12.5, 25 mg/kg
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Administration:i.g. 2 h before anesthetize
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Result:Attenuated SP-induced local paw swelling and Evans blue exudation dose-dependently.
Mitigated SP-induced vasodilation and inhibited mast cell deformation and degranulation.
Reduced plasma histamine concentrations in a dose-dependent manner.
Chemical Information
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CAS No. 724709-67-5
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Appearance Solid
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Masse moléculaire 320.34
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Formule C20H16O4
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Color White to off-white
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SMILES
O=C1C=CC2=C(C3=C(OC=C3)C=C2O1)OCCCC4=CC=CC=C4
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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 : 100 mg/mL (312.17 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 (15.61 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 (15.61 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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 (276 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
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1217 mL | 15.6084 mL | 31.2168 mL | 78.0421 mL |
| 5 mM | 0.6243 mL | 3.1217 mL | 6.2434 mL | 15.6084 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL | 7.8042 mL | |
| 15 mM | 0.2081 mL | 1.0406 mL | 2.0811 mL | 5.2028 mL | |
| 20 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9021 mL | |
| 25 mM | 0.1249 mL | 0.6243 mL | 1.2487 mL | 3.1217 mL | |
| 30 mM | 0.1041 mL | 0.5203 mL | 1.0406 mL | 2.6014 mL | |
| 40 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9511 mL | |
| 50 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL |
BER-5 Related Classifications
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