2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Phosphodiesterase (PDE) Bcl-2 Family NO Synthase Apoptosis
  4. PDE4B/D-IN-5

PDE4B/D-IN-5 (Compound P32) 是一种外周限制性、血脑屏障穿透性极低的、具有口服活性的 PDE4B 和 PDE4D 抑制剂，IC50 分别为 3.4 nM 和 2.2 nM。PDE4B-IN-8 抑制 TNF-α 的产生。PDE4B/D-IN-5 显著降低 Bax/Bcl2 比值、通过降低 MPO 活性和 NO 水平来减轻氧化应激。PDE4B/D-IN-5 具有抗炎、抗氧化和抗凋亡 (Anti-apoptotic) 活性。PDE4B/D-IN-5 可用于急性肺损伤的研究。

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PDE4B/D-IN-5

PDE4B/D-IN-5 Chemical Structure

CAS No. : 3064814-26-9

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PDE4B/D-IN-5 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 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 NO Synthase 亚型特异性产品:

查看所有亚型
nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE4B/D-IN-5 (Compound P32) is a peripherally restricted, oral active inhibitor of PDE4B and PDE4D with extremely low blood-brain barrier penetration, with IC50 values of 3.4 nM and 2.2 nM, respectively. PDE4B-IN-8 inhibits the production of TNF-α. PDE4B/D-IN-5 significantly reduces the Bax/Bcl2 ratio, and alleviates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. PDE4B/D-IN-5 can be used for the research of acute lung injury[1].

IC50 & Target[1]

PDE4B1

3.4 nM (IC50)

PDE4D3

2.2 nM (IC50)

体外研究
(In Vitro)

PDE4B/D-IN-5 可在体外荧光偏振酶活实验中强效抑制重组 PDE4B1 (IC50 = 3.4 nM)[1]。
PDE4B/D-IN-5 (15 μM；最长 90 min) 在大鼠肝微粒体中表现出高代谢稳定性，60 min 后剩余 94.8%，半衰期为 5.5 h，清除率低至 0.0021 mL min−1 mg−1[1]。
PDE4B/D-IN-5 (1-4 μM；1 h) 呈剂量依赖性抑制 LPS 刺激的 RAW264.7 小鼠巨噬细胞中 TNF-α 的产生[1]。

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

PDE4B/D-IN-5 相关抗体:

ELISA Assay[1]

Cell Line: RAW264.7 murine macrophages
Concentration: 1-4 μM
Incubation Time: 1 h
Result: Reduced supernatant TNF-α levels in a dose-dependent manner compared to the LPS-induced model group (which had TNF-α levels of 26 pg/mL, vs baseline 9 pg/mL in untreated cells).
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t AUC0-∞ T1/2 MRT
Mice[1] 1 (plasma) mg/kg i.v. 4.98 min 7665.53 ng/mL 5661.94 ng·h/mL 5735.78 ng·h/mL 1.26 h 1.09 h
Mice[1] 25 (plasma) mg/kg p.o. 36 min 46941.22 ng/mL 111577.48 ng·h/mL 127646.89 ng·h/mL 2.45 h 3.40 h
Mice[1] 1 (brain) mg/kg i.v. 9.98 min 49.69 ng/mL 73.90 ng·h/mL 80.96 ng·h/mL 2.07 h 2.71 h
体内研究
(In Vivo)

PDE4B/D-IN-5 (1-6 mg/kg；口服) 不会诱导比格犬呕吐[1]。
PDE4B/D-IN-5 (6-12 mg/kg；腹腔注射；每日 1 次；连续 5 天) 可通过 cAMP-Epac 通路介导的抗炎、抗氧化及抗凋亡作用，呈剂量依赖性减轻脂多糖 (LPS) 诱导的雄性 C57BL/6 小鼠急性肺损伤[1]。

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

Animal Model: C57BL/6 mice (male, 8 weeks old, acute lung injury model via intratracheal LPS instillation)[1]
Dosage: 6 mg/kg; 12 mg/kg
Administration: i.p.; daily; 5 days
Result: Reduced lung erythema, enlargement, alveolar damage, interstitial edema, and inflammatory cell infiltration.
Showed a significant reduction in Smith lung injury scores in the 12 mg/kg group compared to the model group.
Reduced lung wet/dry weight ratios with a dose-dependent trend.
Reduced bronchoalveolar lavage fluid (BALF) neutrophil counts more effectively than dexamethasone, with a dose-dependent effect.
Attenuated lung myeloperoxidase (MPO) activity more potently than dexamethasone, with a dose-dependent effect.
Reduced lung tissue nitric oxide (NO) levels to values comparable to dexamethasone.
Suppressed BALF tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) levels in a dose-dependent manner, with the 12 mg/kg group showing greater suppression than dexamethasone.
Dose-dependently elevated lung tissue cAMP levels, with the 12 mg/kg group showing the most pronounced effect.
Induced a dose-dependent, significant upregulation of Epac1 protein expression.
Significantly decreased the Bax/Bcl2 ratio, indicating suppression of mitochondrial apoptosis.
Showed no statistically significant changes in p-PKA/PKA or p-AMPK/AMPK ratios.
分子量

425.43

Formula

C22H21F2N5O2
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

PDE4B/D-IN-5 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:

PDE4B/D-IN-53064814-26-9Phosphodiesterase (PDE)Bcl-2 FamilyNO SynthaseApoptosisNitric oxide synthasesNOSPDE4D3cyclic adenosine monophosphateRAW264.7 cellscAMP-Epac pathwayC57BL/6 miceacute lung injuryrat hepatic microsomesPDE4B1tumor necrosis factor-αPDE4BInhibitorinhibitorinhibit

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