(Rac)-PF-184 hydrate |
| Catalog No.GC66334 |
(Rac)-PF-184 수화물은 IC50이 37nM인 B 키나아제 2(IKK-2) 억제제인 강력한 억제 인자-κ입니다. 821d96072c2d58d8970e76f526b0f6b8(Rac)-PF-184 수화물은 항염 효과가 있습니다.821d96072c2d58d8970e76f526b0f6b8
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects[1].
(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].
(Rac)-PF-184 (0.3-2.5 mg; i.t.; once) blocks neutrophil infiltration and BAL cell cytokine production[1].
| 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] |
| Dosage: | 0.3-2.5 mg |
| Administration: | Nano suspension and administered intratracheally in a volume of 100 µL, 60 min before aerosolized LPS |
| 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. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *