型号:
产品价格:电议      采购度:1602      原产地:美洲
发布时间:2021/7/24 0:23:13 所属地区:上海 上海市
简要描述:
WHI-P97 是一种有效的选择性 JAK-3 抑制剂。WHI-P97 在动物模型中有效预防过敏性哮喘的发展。
标签:whi-p97
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CAS No. : 211555-05-4
MCE 站:WHI-P97
产品活性:WHI-P97 是一种有效的选择性 JAK-3 抑制剂。WHI-P97 在动物模型中有效预防过敏性哮喘的发展。
研究领域:Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling
作用靶点:JAK
In Vitro: 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.
In Vivo: 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.
相关产品:Bioactive Compound Library Plus | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | AG490 | Upadacitinib | AT9283 | Gandotinib | Lestaurtinib | Cucurbitacin I | Oclacitinib maleate | JANEX-1 | XL019 | Atractylenolide I | FLLL32 | LFM-A13 | Brevilin A | ZM39923 hydrochloride | Ginsenoside Rk1 | WHI-P154 | Curculigoside | FM-381 | RO8191 | Reticuline | TCS 21311 | Coumermycin A1 | Delphinidin chloride | Ilginatinib maleate | Protosappanin A | Dehydrocrenatidine | FM-479 | NSC 33994 | ZM 449829
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更新时间:2024/1/2 10:14:29
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