2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE4-IN-12

PDE4-IN-12 是一种强效的 PDE4 泛型抑制剂，其对 PDE4 和 PDE7 的 IC50 值分别为 3.5 和 15 nM (SI 分别为 2.71 和 4.27)。PDE4-IN-12 具有较好的安全性，可用于炎症性肠病 (IBDs) 的研究。

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PDE4-IN-12 Chemical Structure

PDE4-IN-12 Chemical Structure

CAS No. : 2901084-32-8

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PDE4-IN-12 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs)[1].

IC50 & Target

PDE4D2

3.51 nM (IC50)

PDE4B2

9.51 nM (IC50)

PDE7A

15 nM (IC50)

PDE5A1

1.24 μM (IC50)

PDE10A

1.02 μM (IC50)

PDE8A1

194 nM (IC50)

体外研究
(In Vitro)

PDE4-IN-12 (compound 22d) (10, 20 µM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect)[1].

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

PDE4-IN-12 相关抗体:

Cell Viability Assay[1]

Cell Line: Raw264.6 cells
Concentration: 10, 20 µM
Incubation Time: 24 h
Result: Reduced the NO release by dose-dependent manner in the LPS induced inflammatory cell model.
体内研究
(In Vivo)

PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium)[1].
PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs[1].
PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T1/2 and AUC0-24 h values of 4.18 h and 6522 hng/mL[1].

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

Animal Model: Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model)[1].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; twice daily for 8 days.
Result: Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.
Animal Model: Beagle dogs[1].
Dosage: 10 mg/kg (solved in 0.5% CMC-Na solution).
Administration: Oral administration; single.
Result: Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.
Animal Model: Male C57BL/6 mice (5 to 6-week old; 15-17 g)[1].
Dosage: 2.5 mg/kg
Administration: Intravenous injection; single.
Result: 1.19 Pharmacokinetic Parameters of PDE4-IN-12 in Male C57BL/6 mice[1].
T1/2 (h) AUC0-24 h (h⋅ng/mL) MRT0-24 h (h) CL (mL/min/kg) Vss (mL/kg)
IV (2.5 mg/kg) 4.18 6522 1.76 6.40 673
分子量

553.64

Formula

C34H35NO6
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

PDE4-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

PDE4-IN-122901084-32-8Phosphodiesterase (PDE)IBDsinflammatory bowelCrohn’s diseaseulcerative colitisRaw264.6Inhibitorinhibitorinhibit

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目录号：
HY-151174
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