PSB-172656
Based on 1 Customer Validation
PSB-172656 is a selective MRGPRX2 antagonist with a Ki of 0.142 nM. PSB-172656 competitively blocks receptor activation by multiple agonists, inhibits Gαq/Gαi dissociation and β-arrestin recruitment, and blocks CXCL14-induced MRGPRX2 calcium mobilization and MRGPRB2 activation. PSB-172656 blocks signaling of the mouse ortholog and mast cell activation, and prevents agonist-induced tracheal contraction, hind paw edema, and systemic anaphylactic symptoms. PSB-172656 can be used for research on mast cell-mediated hypersensitivity and chronic inflammatory diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.24%
- CAS. Nr.: 2641397-91-1
- Formel: C15H15F2N3O
- Molecular Weight:291.30
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
MRGPRX2 0.142 nM (Ki) |
In Vitro
PSB-172656 (100 nM; 30 min) completely blocks CXCL14-induced calcium mobilization in LN229 cells recombinantly expressing MRGPRX2[2].
PSB-172656 blocks CXCL14-induced β-arrestin recruitment in CHO cells recombinantly expressing human MRGPRX2[2].
PSB-172656 (100 nM-1 µM; 30 min) blocks CXCL14-induced MRGPRB2 activation in 1321N1 astrocytoma cells[2].
PSB-172656 is metabolically stable in human liver microsomes with Clint 15 µL/min/mg and estimated half-life 92 min[1].
PSB-172656 (10 µM; 30-90 min) is a competitive, selective MRGPRX2 antagonist in β-arrestin assays, with low-nanomolar Ki values (CST-14 Ki 6.81 nM)[1].
PSB-172656 (0.142 nM (Ki); 30 min) blocks CST-14-induced MRGPRX2-mediated Ca2+ mobilization in LN229-MRGPRX2 cells with Ki 0.142 nM[1].
PSB-172656 (100 nM) completely blocks MRGPRX2-mediated Gαq and Gαi1 activation in LN229-MRGPRX2 cells[1].
PSB-172656 blocks mouse MRGPRB2 in Ca2+ assays with Ki 0.302 nM[1].
PSB-172656 inhibits MRGPRX2-mediated Ca2+ mobilization in human LAD2 mast cells[1].
PSB-172656 (5.26 nM; 5-30 min) inhibits SP-induced β-hexosaminidase release in human LAD2 mast cells with IC50 5.26 nM[1].
PSB-172656 (0.5-10 µM; 30 min) inhibits CST-14-induced degranulation in primary human skin mast cells, with >50% inhibition at 1.25 µM[1].
PSB-172656 (0.01-10 µM; 24-71 h) is non-cytotoxic in 1321N1 astrocytoma cells up to 10 µM[1].
PSB-172656 (30 nM; 5 min) completely prevents SP-induced CD107a and CD63 externalization in LAD2 cells without affecting C3a signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
PSB-172656 (50 mg/kg b.w.; i.p.; single dose; 30 min before i.p. C48/80) suppresses C48/80-induced systemic CCL2 elevation in C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 22-27 g)[1]
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Dosage:50 mg/kg b.w.
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Administration:i.p.; single dose; 30 min before intraplantar C48/80
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Result:Led to a significant decrease in paw swelling compared to controls without the antagonist.
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Animal Model:C57BL/6 (male, 22-27 g)[1]
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Dosage:50 mg/kg b.w.
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Administration:i.p.; single dose; 30 min before i.p. C48/80
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Result:C48/80 elevated plasma CCL2 and IL-8.
Resulted in decreased levels of CCL2.
Chemical Information
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CAS. Nr. 2641397-91-1
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Appearance Solid
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Molecular Weight 291.30
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Formel C15H15F2N3O
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Color Light yellow to light brown
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SMILES
O=C1C(CC)=C(C(C)C)N=C2NC3=CC(F)=C(C=C3N12)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 4 mg/mL (13.73 mM; Need warming; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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: ≥ 0.4 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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: ≥ 0.4 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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.
In Vivo Dissolution Calculator
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 (sealed storage, away from moisture and light)
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.
Protokoll
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
Reinheit & Dokumentation
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Data Sheet (292 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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Handling Instructions (2659 KB)
Verweise
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 (sealed storage, away from moisture and light). 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 | 3.4329 mL | 17.1644 mL | 34.3289 mL | 85.8222 mL |
| 5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL | 17.1644 mL | |
| 10 mM | 0.3433 mL | 1.7164 mL | 3.4329 mL | 8.5822 mL |
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