1. NF-κB
  2. IKK
  3. (Rac)-PF-184 hydrate

(Rac)-PF-184 hydrate 

Cat. No.: HY-107591A Purity: ≥98.0%
Handling Instructions

(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.

For research use only. We do not sell to patients.

(Rac)-PF-184 hydrate Chemical Structure

(Rac)-PF-184 hydrate Chemical Structure

Size Price Stock Quantity
1 mg USD 208 In-stock
Estimated Time of Arrival: December 31
5 mg USD 624 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

(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].

IC50 & Target[1]

IKK-2

37 nM (IC50)

In Vitro

(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(Rac)-PF-184 (0.3-2.5 mg; i.t.; once) blocks neutrophil infiltration and BAL cell cytokine production[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

659.64

Formula

C32H34ClFN6O5

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.[2.25].O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥98.0%

References
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Product Name:
(Rac)-PF-184 hydrate
Cat. No.:
HY-107591A
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