1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. FCPR03

FCPR03 是一种有效的选择性的磷酸二酯酶 4 (PDE4) 抑制剂,对于 PDE4 催化域,PDE4B1PDE4D7IC50 值分别为 60 nM,31 nM 和 47 nM。FCPR03 对 PDE4 的选择性比其他 PDE (PDE1-3 和 PDE5-11) 至少高 2100 倍。FCPR03 具有抗炎,神经保护和抗抑郁样作用。

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FCPR03 Chemical Structure

FCPR03 Chemical Structure

CAS No. : 1917347-65-9

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10 mM * 1 mL in DMSO ¥2640
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects[1][2].

IC50 & Target[1]

PDE4 catalytic domain

60 nM (IC50)

PDE4B1

31 nM (IC50)

PDE4D7

47 nM (IC50)

体外研究
(In Vitro)

FCPR03 (5-20 μM; 30 hours; HT-22 cells) treatment increases cell viability (oxygen-glucose deprivation (OGD)-induced) in a dose-dependent manner, and 10 μM FCPR03 shows significant protective effects[1].
FCPR03 (20 μM; 30 hours; HT-22 cells) treatment protects against OGD-induced cellular apoptosis in both HT-22 cells and cortical neurons. The levels of mitochondrial membrane potential (MMP) and ROS are also restored by FCPR03[1].
FCPR03 (20 μM; 30 hours; HT-22 cells) treatment increases the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin[1].

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

Cell Viability Assay[1]

Cell Line: HT-22 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 30 hours
Result: Increased cell viability in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HT-22 cells
Concentration: 20 μM
Incubation Time: 30 hours
Result: Reversed the effects of OGD and decreased the ratio of apoptotic cells.

Western Blot Analysis[1]

Cell Line: HT-22 cells
Concentration: 20 μM
Incubation Time: 30 hours
Result: Increased the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin.
体内研究
(In Vivo)

FCPR03 (1.25-5 mg/kg; intraperitoneal injection; once; adult male Sprague-Dawley rats) treatment reduces the infarct volume and improves neurobehavioral outcomes in rats following MCAO. FCPR03 increases the levels of phosphorylated AKT, GSK3β and β-catenin within the ischemic penumbra of rats following cerebral ischemia-reperfusion[1].

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

Animal Model: Adult male Sprague-Dawley rats (250-280 g) induced middle cerebral artery occlusion (MCAO)[1]
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration: Intraperitoneal injection; once
Result: Reduced the infarct volume and improved neurobehavioral outcomes in rats following MCAO.
分子量

299.31

Formula

C15H19F2NO3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (334.10 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3410 mL 16.7051 mL 33.4102 mL
5 mM 0.6682 mL 3.3410 mL 6.6820 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3410 mL 16.7051 mL 33.4102 mL 83.5254 mL
5 mM 0.6682 mL 3.3410 mL 6.6820 mL 16.7051 mL
10 mM 0.3341 mL 1.6705 mL 3.3410 mL 8.3525 mL
15 mM 0.2227 mL 1.1137 mL 2.2273 mL 5.5684 mL
20 mM 0.1671 mL 0.8353 mL 1.6705 mL 4.1763 mL
25 mM 0.1336 mL 0.6682 mL 1.3364 mL 3.3410 mL
30 mM 0.1114 mL 0.5568 mL 1.1137 mL 2.7842 mL
40 mM 0.0835 mL 0.4176 mL 0.8353 mL 2.0881 mL
50 mM 0.0668 mL 0.3341 mL 0.6682 mL 1.6705 mL
60 mM 0.0557 mL 0.2784 mL 0.5568 mL 1.3921 mL
80 mM 0.0418 mL 0.2088 mL 0.4176 mL 1.0441 mL
100 mM 0.0334 mL 0.1671 mL 0.3341 mL 0.8353 mL
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.

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FCPR03
目录号:
HY-117977
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