For research use only. Not for use in humans.
Catalog No.S8804 Synonyms: PF-841
Molecular Weight(MW): 389.40
PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
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|Description||PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.|
The pharmacokinetics of PF-06700841 are studied in Sprague−Dawley rats following intravenous and oral administration (1 and 3 mg/kg respectively) of the tosylate salt, where the compound shows a plasma clearance of 31 mL/min/kg, a volume of distribution of 2.0 L/kg, and oral bioavailability of 83%. Following the 3 mg/kg oral dose, the Cmax is 774 ng/mL and the AUC∞ is 1340 ng·h/mL. The high oral bioavailability indicates high absorption from the gut, consistent with its in vitro passive permeability properties and high solubility.
|In vitro||DMSO||78 mg/mL (200.3 mM)|
|Ethanol||78 mg/mL (200.3 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04090047||Not yet recruiting||Drug: PF-06700841|Drug: Itraconazole||Healthy Participants||Pfizer||September 16 2019||Phase 1|
|NCT03656952||Completed||Drug: PF-06700841|Drug: Placebo|Drug: moxifloxacin||Healthy||Pfizer||September 5 2018||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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