I-BET787
Based on 1 Customer Validation
I-BET787 is a orally active BET bromine domain inhibitor with pIC50s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice.
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- Pureté : 99.88%
- CAS No.: 2201082-98-4
- Formule: C16H20ClN3O2
- Masse moléculaire:321.80
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Stockage:
RT, sealed storage, away from moisture and light.
In solvent -80°C, 1 year , -20°C, 6 months
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
BRD4 BD1 7.1 (pIC50) |
BRD4 BD2 5.9 (pIC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 mice are received a single bolus intraperitoneal (IP) administration of trinitrophenol-keyhole limpet hemocyanin (100 μg/kg)[1]
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Dosage:1.5, 5, or 15 mg/kg
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Administration:p.o; once every day (QD) or twice every day (BID) over a 14 day
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Result:Mouse body weights were not significantly affected across the 14 days.
Demonstrated efficacy in a mouse model of inflammation.
Chemical Information
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CAS No. 2201082-98-4
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Appearance Solid
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Masse moléculaire 321.80
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Formule C16H20ClN3O2
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Color White to off-white
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SMILES
CC1=CC(C2=NC(Cl)=CN2CC3CCOCC3)=CN(C1=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
RT, sealed storage, away from moisture and light
In solvent -80°C 1 year -20°C 6 months
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (310.75 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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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].
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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
Pureté et documentation
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Fiche technique (276 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
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1075 mL | 15.5376 mL | 31.0752 mL | 77.6880 mL |
| 5 mM | 0.6215 mL | 3.1075 mL | 6.2150 mL | 15.5376 mL | |
| 10 mM | 0.3108 mL | 1.5538 mL | 3.1075 mL | 7.7688 mL | |
| 15 mM | 0.2072 mL | 1.0358 mL | 2.0717 mL | 5.1792 mL | |
| 20 mM | 0.1554 mL | 0.7769 mL | 1.5538 mL | 3.8844 mL | |
| 25 mM | 0.1243 mL | 0.6215 mL | 1.2430 mL | 3.1075 mL | |
| 30 mM | 0.1036 mL | 0.5179 mL | 1.0358 mL | 2.5896 mL | |
| 40 mM | 0.0777 mL | 0.3884 mL | 0.7769 mL | 1.9422 mL | |
| 50 mM | 0.0622 mL | 0.3108 mL | 0.6215 mL | 1.5538 mL | |
| 60 mM | 0.0518 mL | 0.2590 mL | 0.5179 mL | 1.2948 mL | |
| 80 mM | 0.0388 mL | 0.1942 mL | 0.3884 mL | 0.9711 mL | |
| 100 mM | 0.0311 mL | 0.1554 mL | 0.3108 mL | 0.7769 mL |
I-BET787 Related Classifications
HY-163729 Related Classifications
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