Brepocitinib (PF-06700841)

Brepocitinib (PF-06700841, PF-841) 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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5mg

￥950.00

760.00

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25mg

￥3250.00

2600.00

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货号: ajci23052
CAS: 1883299-62-4
别名: PF-841
分子式: C18H21F2N7O
分子量: 389.4
纯度: >98%
溶解度: DMSO: 78 mg/mL (200.31 mM);Water: Insoluble;Ethanol: 78 mg/mL (200.31 mM)
储存: Store at -20°C
库存: 现货

Background

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[1].

[1] Fensome A, et al. J Med Chem. 2018, 61(19):8597-8612.