2. Metabolic Enzyme/Protease Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Phosphodiesterase (PDE) Interleukin Related CXCR TNF Receptor
  4. PDE4D inhibitor 1

PDE4-IN-1 是一种 PDE4 抑制剂，具有高效价 (IC50：8.6 nM) 且优于其他 PDE 亚型的选择性。PDE4-IN-1 可抑制炎性细胞因子和趋化因子的释放。PDE4-IN-1 可显著修复受损的 cAMP-CREB 信号通路。PDE4-IN-1 可抑制增殖并促进分化，从而逆转银屑病的形成。

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PDE4D inhibitor 1 Chemical Structure

PDE4D inhibitor 1 Chemical Structure

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PDE4D inhibitor 1 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 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 CXCR 亚型特异性产品:

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a 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

PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis[1].

IC50 & Target[1]

PDE4B1

5.3 nM (IC50)

PDE4D2

8.6 nM (IC50)

PDE4A10

100 nM (IC50)

PDE4C1

747 nM (IC50)

PDE5A1

1730 nM (IC50)

PDE10A2

1953 nM (IC50)

PDE7A1

5913 nM (IC50)

PDE1B2

>10000 nM (IC50)

PDE2A

>10000 nM (IC50)

PDE3A

>10000 nM (IC50)

PDE8A1

>10000 nM (IC50)

PDE9A2

>10000 nM (IC50)

体外研究
(In Vitro)

PDE4-IN-1 (Compound L30) (5-20 μM，2 小时) 可降低 LPS 诱导的 Raw264.7 细胞中炎症细胞 (IL-1β、IL-6 和 TNF-α) 的 mRNA 水平[1]。
PDE4-IN-1 (5-20 μM，24 小时) 可降低 M5 刺激的 HaCaT 细胞中炎症细胞因子 (CXCL-2、IL-17 和 TNF-α) 的 mRNA 水平[1]。
PDE4-IN-1 (0-20 μM，24 小时) 可抑制 M5 刺激的 HaCaT 细胞增殖[1]。
PDE4-IN-1 (20 μM，24 小时) 可降低 M5 刺激的 HaCaT 细胞中 K6 和 K17 的蛋白表达，同时上调分化相关蛋白 K1 和 K10 的表达[1]。
PDE4-IN-1 (20 μM，2 小时) 与 Roflumilast (HY-15455) 联合使用可恢复 M5 刺激的 HaCaT 细胞中的 cAMP 水平，并增强下游 CREB 的磷酸化[1]。
PDE4-IN-1 (0-80 μM，24 小时) 对 RAW264.7 和 HaCaT 细胞表现出较低的细胞毒性[1]。

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

PDE4D inhibitor 1 相关抗体:
体内研究
(In Vivo)

PDE4-IN-1 (Compound L30) (0.3%软膏-100mg，局部给药，7 天) 可缓解银屑病症状，减轻皮肤红斑的严重程度。[1]

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

Animal Model: Female BALB/c mice models (6-8 weeks old, weighing 20-22 g each, a total of 40 mice) with 5% IMQ-containing cream for 7 days [1]
Dosage: 0.3% ointment-100 mg
Administration: Topical administrations
Result: Alleviated psoriatic symptoms and was more potent to decrease the thickness, scales, and erythema scores than Roflumilast (20 mg/kg) in the last 4 days.
Downregulated inflammatory cytokines and chemotaxis such as TNF-α, IL-1β, IL-6, IL-17, CXCL-2, and CCL-20.
Reduced protein expression of K6 and K17.
Reversed expression level of K1 and K10.
Exerted antipsoriasis effects by inhibiting the excessive proliferation and promoting poor differentiation.
Partly reversed the body weight loss and reduced skin thickness induced by IMQ suggesting low risk of toxicity in vivo.
分子量

489.47

Formula

C25H25F2NO7
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

PDE4D inhibitor 1 相关分类

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  • 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:

PDE4D inhibitor 1Phosphodiesterase (PDE)Interleukin RelatedCXCRTNF ReceptorILCXC chemokine receptorsC-X-C motif chemokine receptorsTumor Necrosis Factor ReceptorTNFRPDE4anti-inflammatoryanti-psoriasiscAMPCREBRaw264.7 cellsHaCaT cellIMQpsoriatic modelBALB/c miceInhibitorinhibitorinhibit

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