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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