WHI-P97

Research use only, not for human use.

A potent, specific JAK3 inhibitor with Ki of 0.6-2.3 uM.

A potent, specific JAK3 inhibitor with Ki of 0.6-2.3 uM; inhibits the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and inhibits mast cell leukotriene synthesis in vitro; shows promising biological activity in mouse model of allergic asthma.

WHI-P97 inhibits the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcεRI crosslinking by >90% at low micromolar concentrations.WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells.

WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD10 is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose.WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t1/2 of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and Cmax are 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC50 values are 58.4 μM and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution are 322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice.WHI-P97 (intraperitoneal injection; 40 mg/kg; 24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion. Animal Model:BALB/c mouse model of allergic asthmaDosage:40 mg/kg Administration:intraperitoneal injection; 24 days Result:Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels.

WHI-P-97 | WHI P97

Angiogenesis

JAK

JAK3

Cancer

——

211555-05-4

455.1007

C16H13Br2N3O3

>98% (HPLC)

10 mM in DMSO

OC1=C(Br)C=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1Br

Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-

(-20℃)

With Ice Pack

≥ 2 years