FR173657
Based on 1 Customer Validation
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease.
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- Pureza : 99.00%
- No. CAS: 167838-64-4
- Fòrmula: C30H27Cl2N5O4
- Peso molecular:592.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.4 nM
Compound: 87b
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Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
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[PMID: 9767643] |
| CHO | IC50 |
1.4 nM
Compound: 5
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Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
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[PMID: 9804698] |
| HEK293 | IC50 |
1.4 nM
Compound: 1, FK-3657
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Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
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[PMID: 19552431] |
| MDA-MB-231 | IC50 |
20 μM
Compound: FR-173657
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
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[PMID: 33139111] |
Chemical Information
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No. CAS 167838-64-4
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Appearance Solid
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Peso molecular 592.47
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Fòrmula C30H27Cl2N5O4
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Color White to off-white
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SMILES
O=C(NCC(N(C1=CC=C(Cl)C(COC2=C3N=C(C)C=CC3=CC=C2)=C1Cl)C)=O)/C=C/C4=CC=C(NC(C)=O)N=C4
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Synonyms
FK-3657
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 33.33 mg/mL (56.26 mM; ultrasonic and warming and heat to 60°C; 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)
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: ≥ 3.33 mg/mL (5.62 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
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.
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
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Ficha de datos (269 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.6878 mL | 8.4392 mL | 16.8785 mL | 42.1962 mL |
| 5 mM | 0.3376 mL | 1.6878 mL | 3.3757 mL | 8.4392 mL | |
| 10 mM | 0.1688 mL | 0.8439 mL | 1.6878 mL | 4.2196 mL | |
| 15 mM | 0.1125 mL | 0.5626 mL | 1.1252 mL | 2.8131 mL | |
| 20 mM | 0.0844 mL | 0.4220 mL | 0.8439 mL | 2.1098 mL | |
| 25 mM | 0.0675 mL | 0.3376 mL | 0.6751 mL | 1.6878 mL | |
| 30 mM | 0.0563 mL | 0.2813 mL | 0.5626 mL | 1.4065 mL | |
| 40 mM | 0.0422 mL | 0.2110 mL | 0.4220 mL | 1.0549 mL | |
| 50 mM | 0.0338 mL | 0.1688 mL | 0.3376 mL | 0.8439 mL |
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