2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphodiesterase (PDE) TNF Receptor
  4. LY2775240

LY2775240 是一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4A (IC₅₀ = 0.09 nM)、PDE4B (IC₅₀ = 0.09 nM) 和 PDE4D (IC₅₀ = 0.14 nM) 的抑制活性较强，对 PDE4C 的 IC₅₀ 为 2.4 nM。LY2775240 是一种高选择性试剂，可在免疫激活时减少 TNFα 的产生。LY2775240 可在啮齿类和恒河猴模型中降低 TNFα 的产生。LY2775240 可用于银屑病的研究。

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LY2775240

LY2775240 Chemical Structure

CAS No. : 1628160-15-5

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LY2775240 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY2775240 is an orally available phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC₅₀ = 0.09 nM), PDE4B (IC₅₀ = 0.09 nM), and PDE4D (IC₅₀ = 0.14 nM), and exhibits an IC₅₀ of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production during immune activation. It effectively lowers TNFα levels in rodent and cynomolgus monkey models. LY2775240 can be used in research on psoriasis[1].

IC50 & Target[1]

PDE4A

0.09 nM (IC50)

PDE4B

0.09 nM (IC50)

PDE4D

0.14 nM (IC50)

PDE4C

2.4 nM (IC50)

体外研究
(In Vitro)

LY2775240 可强效抑制人全血中 LPS (HY-D1056) 诱导的 TNFα 分泌，其 IC50 为 18 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LY2775240 相关抗体:
体内研究
(In Vivo)

LY2775240 (3-10 mg/kg；灌胃；单次给药) 可显著降低小鼠体内 LPS 诱导的 TNFα 产生[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6 (female, 8–10 weeks old, LPS-induced)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced plasma TNFα to 53% of vehicle control at 3 mg/kg; reduced plasma TNFα to 35% of vehicle control at 10 mg/kg.
分子量

485.58

Formula

C26H35N3O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LY2775240 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY27752401628160-15-5LY 2775240LY-2775240Phosphodiesterase (PDE)TNF ReceptorTumor Necrosis Factor ReceptorTNFRPDE4CPDE4BpsoriasisPDE4Drodent modelsTNFαPDE4Arhesus monkey modelsphosphodiesterase 4PDE4Inhibitorinhibitorinhibit

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HY-201403
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