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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
PF-03394197 maleate
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1640292-55-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1089.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥350.0 |
| 规格： | 5 mg | 产品价格： | ￥990.0 |
| 规格： | 10 mg | 产品价格： | ￥1450.0 |
| 规格： | 50 mg | 产品价格： | ￥4900.0 |
| 规格： | 100 mg | 产品价格： | ￥7900.0 |
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Oclacitinib maleate
CAS No. : 1640292-55-2
MCE 国际站：Oclacitinib maleate
产品活性：Oclacitinib maleate (PF-03394197 maleate) 是一种新型 JAK 抑制剂。Oclacitinib maleate (PF-03394197 maleate) 抑制 JAK1 最有效，IC50 为 10 nM。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点：JAK
In Vitro: Using isolated enzyme systems and in vitro human or canine cell models, potency and selectivity of Oclacitinib is determined against JAK family members and cytokines that trigger JAK activation in cells. Inhibitory activity of Oclacitinib against JAK family members is determined in isolated enzyme systems. Oclacitinib inhibits JAK1, JAK2, JAK3, and TYK2 by 50% at concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively. Oclacitinib is most potent against the JAK1 enzyme, showing a 1.8-fold selectivity for JAK1 vs. JAK2 and 9.9-fold selectivity toward JAK1 vs. JAK3. Oclacitinib inhibits JAK family members by 50% at concentrations (IC50's) ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases (IC50's >1000 nM). Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50's ranging from 36 to 249 nM. Oclacitinib has minimal effects on cytokines that does not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's >1000 nM).Topical treatment with Tofacitinib (0.1%) and Oclacitinib (0.1%) leads to significant reduction of cell migration from mouse ear explants compared with vehicle-treated ears (all P < 0.05). The cell counts of MHC class II positive cells (that is, Langerhans cells) are significantly lower in vehicle-treated compared with each JAK inhibitor–treated epidermis (all P<0.01).
In Vivo: Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01). Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus and a presumptive diagnosis of allergic dermatitis are enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h.
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文献和实验sodium maleate pH 5.2 (3 x 5'). 8). en bloc stain in 1% uranyl acetate in maleate buffer pH 5.2 (1 hr RT). Using uranyl acetate at low pH will improve membrane contrast. Analternative contrasting method, which adds even more membrane contrast
糖液500ml稀释后缓慢滴入。 马来酸麦角新碱（ergometrine maleate）口服，0.2～0.5mg/次。肌内注射，0.2～0.5mg/次，必要时半小时后重复一次。静脉滴注0.2mg以5%葡萄糖溶液稀释后应用。极量：肌内或静脉注射，0.5mg/次，1mg/日。 酒石酸麦角胺（ergotamine tartrate）口服1mg/次。皮下或肌内注射，0.25mg/次。 麦角胺咖啡因片 每片含酒石酸麦角胺1mg，咖啡因100mg。偏头痛发作时即口服半片至1片半；如无效，可于
滴注5～10U/次，可用5%葡萄糖液500ml稀释后缓慢滴入。 马来酸麦角新碱（ergometrine maleate）口服，0.2～0.5mg/次。肌内注射，0.2～0.5mg/次，必要时半小时后重复一次。静脉滴注0.2mg以5%葡萄糖溶液稀释后应用。极量：肌内或静脉注射，0.5mg/次，1mg/日。 酒石酸麦角胺（ergotamine tartrate）口服1mg/次。皮下或肌内注射，0.25mg/次。 麦角胺咖啡因片 每片含酒石酸麦角胺1mg，咖啡因100mg。偏头痛发作
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