2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE5-IN-1

PDE5-IN-1 (compound 2) 是一种 PDE5 抑制剂，其 IC50 为 5.6 nM，且具备口服生物利用度。PDE5-IN-1 可与 PDE5 催化结构域中的 Q817 残基形成氢键相互作用，与 F820 残基形成芳香族 π-π 堆积相互作用。PDE5-IN-1 具有抗心肌肥厚和血管舒张作用，可降低平均肺动脉压及右心室肥厚指数。PDE5-IN-1 可用于肺动脉高压的研究。

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PDE5-IN-1

PDE5-IN-1 Chemical Structure

CAS No. : 2109805-65-2

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PDE5-IN-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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE5-IN-1 (compound 2) is a PDE5 inhibitor with an IC50 of 5.6 nM and oral bioavailability. PDE5-IN-1 forms hydrogen bond interactions with the Q817 residue in the catalytic domain of PDE5, and aromatic π-π stacking interactions with the F820 residue. PDE5-IN-1 exerts anti-cardiac hypertrophy and vasodilatory effects, reduces mean pulmonary arterial pressure and right ventricular hypertrophy index. PDE5-IN-1 can be used in the research of pulmonary arterial hypertension[1].

体外研究
(In Vitro)

PDE5-IN-1 (compound 2) (多浓度；孵育 15 min) 可强效抑制 PDE5A 催化结构域，其 IC50 为 5.6 nM[1]。
PDE5-IN-1 (多浓度；15 分钟) 对 PDE5A 表现出相较于其他 PDE 家族的显著选择性，选择性指数范围为 10 (相对于 PDE6A) 至＞1700 (相对于 PDE1B、PDE3A、PDE7A1、PDE9A2)[1]。
PDE5-IN-1 (多浓度) 对人类主要肝脏 CYP 同工酶仅具有微弱的抑制作用，其中仅对 CYP1A2 有中度抑制作用 (IC50 = 7.6 μM)，而对其他六种关键同工酶无显著抑制作用[1]。
PDE5-IN-1 (多浓度) 对 hERG 钾通道表现出弱抑制作用，其 IC50 >10 μM[1]。
PDE5-IN-1 (0.5 μM; incubated to determine T1/2) 在大鼠和人肝微粒体中均稳定，其半衰期显著长于阳性对照咪达唑仑[1]。

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

PDE5-IN-1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ MRT0-t Tmax Bioavailability
Rat[1] 5 mg/kg p.o. 5.17 h 368 ng/mL 1997 ng·h/mL 2031 ng·h/mL 4.76 h 4.00 h 63.4 %
Rat[1] 2.5 mg/kg i.v. 6.02 h 2359 ng/mL 1703 ng·h/mL 1732 ng·h/mL 2.14 h / /
体内研究
(In Vivo)

PDE5-IN-1 (compound 2) (5.0 mg/kg，灌胃，每日 1 次，连续 3 周) 可在野百合碱 (MCT) 诱导的肺动脉高压 (PAH) 大鼠中显著降低 mPAP 和 RVHI，且其疗效优于 10.0 mg/kg 的枸橼酸西地那非[1]。

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

Animal Model: Wister rats (8 weeks old, 180-220 g, MCT-induced PAH)[1]
Dosage: 5.0 mg/kg
Administration: p.o.; daily; 3 weeks
Result: Reduced mean pulmonary artery pressure (mPAP) to 18.65 mmHg, a statistically significant decrease compared to the PAH model group's 32.74 mmHg.
Reduced right ventricle hypertrophy index (RVHI) to a statistically significant level compared to the model group.
Exhibited better effects on both mPAP and RVHI than sildenafil citrate at 10.0 mg/kg.
分子量

402.42

Formula

C22H14N2O4S
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

PDE5-IN-1 相关分类

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  • 稀释计算器

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  • 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-12109805-65-2Phosphodiesterase (PDE)hERGratsPDE5cytochromePDE5AF820Q817PDE5 catalytic domainpulmonary arterial hypertensionhuman liver microsomesInhibitorinhibitorinhibit

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