| 中文名称: | 奥拉替尼马来酸盐 | ||||
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| 英文名称: | Oclacitinib maleate | ||||
| 别名: | PF-03394197 maleate | ||||
| CAS No: | 1640292-55-2 | 分子式: | C15H23N5O2S.C4H4O4 | 分子量: | 453.51 |
| CAS No: | 1640292-55-2 | ||||
| 分子式: | C15H23N5O2S.C4H4O4 | ||||
| 分子量: | 453.51 | ||||
基本信息
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产品编号： |
O10235 |
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产品名称： |
Oclacitinib maleate |
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CAS: |
1640292-55-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
453.51 |
-20℃ |
1个月 |
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化学名： |
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Solubility (25°C)： |
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体外:
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DMSO |
90mg/mL (198.45mM) |
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Ethanol |
90mg/mL (198.45mM) |
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Water |
18mg/mL (39.69mM) |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.2050mL |
11.0251mL |
22.0502mL |
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5mM |
0.4410mL |
2.2050mL |
4.4100mL |
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10mM |
0.2205mL |
1.1025mL |
2.2050mL |
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50mM |
0.0441mL |
0.2205mL |
0.4410mL |
生物活性
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产品描述 |
一种新型JAK抑制剂。Oclacitinib maleate (PF-03394197 maleate)抑制JAK1最有效，IC50为10nM。 |
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靶点 |
JAK1 |
JAK2 |
TYK2 |
JAK3 |
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10nM |
18nM |
84nM |
99nM |
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体外研究 |
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 84nM,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 99nM and does not inhibit a panel of 38 non-JAK kinases (IC50's >1000nM).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 249nM.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>1000nM).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). |
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体内研究 |
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 0.4-0.6mg/kg orally twice daily or an excipientmatched 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 24h. |
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推荐实验方法(仅供参考)
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激酶实验： |
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Recombinant human active kinase domains for JAK1,JAK2,JAK3,and TYK2 are used in isolated enzyme assays using Caliper microfluidics technology to determine potency of Oclacitinib against the JAK family members.Sequence homology to the analogous sequences in the canine JAK enzymes are 98,98,100,and 90%,respectively.Invitrogen kinase panel testing is performed to determine potency of Oclacitinib toward 38 different non-JAK kinases using their SelectScreen Kinase Profiling Services.Oclacitinib is evaluated at a concentration of 1μM. |
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动物实验: |
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Mice BALB/cAnN (female, 6 weeks old) are used.The JAK inhibitors (Tofacitinib or Oclacitinib) are administered orally or topically 30 minutes before and 4 hours after toluene-2,4-diisocyanate (TDI) challenge because the absorption of Tofacitinib and Oclacitinib is rapid,with plasma concentrations for both Tofacitinib and Oclacitinib peaking at around 1 hour after oral or intravenous administration.Tofacitinib and Oclacitinib both have a short half-life of 2 and 4 hours after administration,respectively.Each drug is diluted in a 0.5% methylcellulose/0.25% Tween 20 solution for oral administration, and a 7:1 acetone:DMSO solution for topical application to concentrations described subsequently. For each drug,a vehicle-only control group and low-and high-dose groups are set.Oral doses are as follows:Tofacitinib,10 and 30mg/kg;and Oclacitinib,30 and 45mg/kg.Topically administered doses are 0.1,0.25,and 0.5% for both chemicals.The oral doses of Tofacitinib and Oclacitinib used in this study are selected. Dogs Dogs are randomized to one of two treatment groups (i.e.Oclacitinib or placebo) in a 1:1 ratio.Dogs in the Oclacitinib treatment group are given Oclacitinib maleate caplets orally at a dose of 0.4-0.6mg/kg twice daily.The scored caplets are provided in three strengths containing 3.6,5.4 and 16mg of Oclacitinib.Dogs in the placebo treatment group are given the same number of caplets,identical in appearance to Oclacitinib maleate caplets and containing all of the same excipients except Oclacitinib maleate. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
