(Rac)-PF-184
(Rac)-PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 has anti-inflammatory effects.
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- CAS. Nr.: 1187460-81-6
- Formel: C32H32ClFN6O4
- Molecular Weight:619.09
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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IKK-2 37 nM (IC50) |
(Rac)-PF-184 has slow dissociation kinetics with a T1/2 of 6.7 h from rhIKK-2, very low oral bioavailability (5%), high intravenous clearance (59 ml/min/kg), and high P450 metabolism in human liver microsomes[1].
(Rac)-PF-184 binds tightly to endogenous IKK-2 and shows extended inhibition of kinase activity and cytokine production[1].
(Rac)-PF-184 shows a concentration-dependent inhibition on LPS- and IL-1β-induced production of inflammatory mediators in a variety of human disease-relevant cells[1].
(Rac)-PF-184 (0.001-10 µM, 1 h) inhibits IL-1β-induced TNF-α in a concentration-dependent manner with maximal efficacies of 94% and relative potencies of 163 nM[1].
(Rac)-PF-184 inhibits LPS-induced cytokine production from rat alveolar macrophages and blocked p65 nuclear translocation[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:Fasted male Sprague-Dawley rats (350 g) placed into a chamber connected to a large volume nebulizer filled with 20 ml of 1 mg/mL solution of LPS[1]
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Dosage:0.3-2.5 mg
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Administration:Nano suspension and administered intratracheally in a volume of 100 µL, 60 min before aerosolized LPS
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Result:Resulted in a comparable attenuation of total cell and PMN cell infiltration 4 h after LPS exposure. Dose-dependently inhibited cell infiltration with EC50 values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity.
Chemical Information
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CAS. Nr. 1187460-81-6
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Molecular Weight 619.09
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Formel C32H32ClFN6O4
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SMILES
O=C(C1=NN(C2=C1CCC3=C2C=C(NC(C4=CC(N5CC(CO)(C(CO)(C5)C)C)=NC=C4Cl)=O)C=C3)C6=CC=C(C=C6)F)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(Rac)-PF-184 Related Classifications
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