| 中文名称 |
Difamilast
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| 英文名称 |
Difamilast
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| 英文别名 |
Difamilast;T3U32GLJ0F;Difamilast [USAN];Difamilast (JAN/USAN);MM36;GTPL9776;BDBM389126;USRE46792, 352;DB14987;example 352 [WO2007058338];D11314;N-[2-(4-difluoromethoxy-3-isopropoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide;N-((2-(4-(difluoromethoxy)-3-(propan-2-yloxy)phenyl)-1,3-oxazol-4-yl)methyl)-2-ethoxybenzamide;N-[[2-[4-(difluoromethoxy)-3-propan-2-yloxyphenyl]-1,3-oxazol-4-yl]methyl]-2-ethoxybenzamide;Benzamide, N-((2-(4-(;N-[[2-[4-(Difluoromethoxy)-3-(1-methylethoxy)phenyl]-4-oxazolyl]methyl]-2-ethoxybenzamide (ACI);MM 36;N-({2-[4-(difluoromethoxy)-3-(propan-2-yloxy)phenyl]-1,3-oxazol-4-yl}methyl)-2-ethoxybenzamide;OPA 15406
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| Cas No. |
937782-05-3
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| 分子式 |
C23H24F2N2O5
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| 分子量 |
446.44
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| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
Difamilast (OPA-15406) 是一种局部的,具有选择性的非甾体磷酸二酯酶 4 (PDE4) 抑制剂,对 B 亚型具有特别有效的抑制作用 (IC50=11.2 nM)。Difamilast 可用于研究轻度至中度特应性皮炎 (AD)。
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| 产品详情 |
Difamilast (OPA-15406) 是一种局部的,具有选择性的非甾体磷酸二酯酶 4 (PDE4) 抑制剂,对 B 亚型具有特别有效的抑制作用 (IC50=11.2 nM)。Difamilast 可用于研究轻度至中度特应性皮炎 (AD)。
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| 生物活性 |
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC 50 =11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).
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| 性状 |
Solid
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| IC50 & Target[1][2] |
PDE4B 11.2 nM (IC50)
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| 体外研究(In Vitro) |
OPA-15406 is highly selective for inhibition of PDE4 subtype B (IC50=11.2 nM), and OPA-15406 also exerts inhibitory effects on PDE2. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
OPA-1540 improves skin condition in relevant animal models of AD. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| ClinicalTrial |
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| 参考文献 |
[1]. Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-con[2]. Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (223.99 mM; Need ultrasonic)配制储备液
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[1]. Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-con[2]. Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。