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

PDE5-IN-2 

目录号: HY-112704
产品使用指南

PDE5-IN-2 是一种有效、高度选择性、可口服的 PDE5 抑制剂,IC50 值为 0.31 nM,对 PDE2A,PDE10A,PDE4D2 和 PDE6C 的选择性相对较弱,IC50 值分别为 106,46,43,1.2 nM。抗肺动脉高压作用。

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PDE5-IN-2 Chemical Structure

PDE5-IN-2 Chemical Structure

CAS No. : 2244517-61-9

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Description

PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].

IC50 & Target[1]

PDE5A1

0.31 nM (IC50)

PDE6C

1.2 nM (IC50)

PDE4D2

43 nM (IC50)

PDE10A

46 nM (IC50)

PDE2A

106 nM (IC50)

In Vitro

PDE5-IN-2 (Compound 3) has at least 1000-fold selectivity over PDE1B, PDE3A, PDE7A1, PDE8A1, and PDE9A2 (IC50s, >32 000 nM)[1].

In Vivo

PDE5-IN-2 (1.25 mg/kg, p.o.) shows anti-pulmonary arterial hypertension activity, decreases mean pulmonary artery pressure in rats[1].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

491.52

Formula

C₂₅H₂₁N₃O₆S

CAS No.

2244517-61-9

SMILES

O=C1C2=C(C3=NC=CS3)NC(CC4=CC(OCO5)=C5C=C4)=C2OC6=CC(NCCOC)=CC(O)=C61

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
PDE5-IN-2
目录号:
HY-112704
需求量:

PDE5-IN-2

Cat. No.: HY-112704