2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE5-IN-13

PDE5-IN-13 抑制磷酸二酯酶 5 (PDE5A)，IC50为 3 nM。PDE5-IN-13 对治疗肺动脉高压有潜在疗效。PDE5-IN-13 与 PDE1，PDE2，PDE3，PDE4，PDE7，PDE8，PDE9，PDE10 和 PDE11 相比，对靶点具有高选择性。PDE5-IN-13 具有合理的药物样特征。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PDE5-IN-13 Chemical Structure

PDE5-IN-13 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

PDE5-IN-13 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

PDE5-IN-13 inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for the treatment of PAH (pulmonary arterial hypertension). PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 has reasonable drug-like profiles[1].

IC50 & Target[1]

PDE5A

3 nM (IC50)

PDE1C

10478 nM (IC50)

PDE2A

3378 nM (IC50)

PDE3A

>100000 nM (IC50)

PDE4D2

53294 nM (IC50)

PDE6C

20 nM (IC50)

PDE7A

25746 nM (IC50)

PDE8A1

>100000 nM (IC50)

PDE9A2

>100000 nM (IC50)

PDE10A2

21160 nM (IC50)

PDE11A

>100000 nM (IC50)

体外研究
(In Vitro)

PDE5-IN-13 的 C3 氰化物基团通过水分子与 D76 4和 H613 形成氢键桥，这稳定了 PDE5-IN-13 结合构象[1]。

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

PDE5-IN-13 相关抗体:
体内研究
(In Vivo)

PDE5-IN-13 (1500 mg/kg, p.o.) 在鼠中无急性毒性[1]。
PDE5-IN-13 (5.0 mg/kg, p.o. , 每天, 21天) 在 Monocrotalin (HY-N0750) 诱导的肺动脉高压大鼠模型中，对增加 mPAP (肺动脉高压) 和 减少 RVHI (右心室肥大指数) 的药效比 Sildenafil citrate (HY-15025A) (10.0mg/kg) 好得多[1]。
PDE5-IN-13 的体内药代动力学特性。

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

PK parameters i.v. administration (2 mg/kg) p.o. administration (10mg/kg)
AUC(0-t)(ng/mL・h) 398.9 338.8
AUC (0−∞)(ng/mL・h) 399.0 340.5
AUC (0−t)(h) 0.75 6.3
AUC (0−∞)(h) 0.76 6.4
t1/2 (h) 2.25 2.79
Tmax (h) 0.083 4.0
CL (L/h/kg) 5.0 31.5
Vz (L/kg) 16.3 126.6
Cmax (ng/mL) 985.2 58.4
F (%) 16.8
分子量

486.56

Formula

C31H26N4O2
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

PDE5-IN-13 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 *
= × ×

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)
× = ×
C1   V1   C2   V2
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:

PDE5-IN-13Phosphodiesterase (PDE)pulmonary arterial hypertension (PAH)inhibitory activitypharmacodynamicInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-170435
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