PDE5-IN-1
PDE5-IN-1 is an orally active, selective PDE5 inhibitor with an IC50 of 5.6 nM. 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.
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- CAS No.: 2109805-65-2
- Formule: C22H14N2O4S
- Masse moléculaire:402.42
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
PDE5-IN-1 (compound 2) (15 min) shows remarkable selectivity for PDE5A over other PDE families, with selectivity indices ranging from 10 (vs PDE6A) to >1700 (vs PDE1B, PDE3A, PDE7A1, PDE9A2)[1].
PDE5-IN-1 has weak inhibitory effects on major human hepatic CYP isoenzymes, with only moderate inhibition of CYP1A2 (IC50 = 7.6 μM) and no significant inhibition of six other key isoenzymes[1].
PDE5-IN-1 shows weak inhibition of the hERG potassium channel, with an IC50 >10 μM[1].
PDE5-IN-1 (0.5 μM) is stable in both rat and human liver microsomes, with significantly longer half-lives than the positive control midazolam[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wister rats (8 weeks old, 180-220 g, MCT-induced PAH)[1]
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Dosage:5.0 mg/kg
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Administration:p.o.; daily; 3 weeks
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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.
Chemical Information
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CAS No. 2109805-65-2
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Masse moléculaire 402.42
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Formule C22H14N2O4S
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SMILES
O=C1C=2C=CC=CC2OC=3C1=C(NC3CC4=CC=C5OCOC5=C4)C6=NC=CS6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE5-IN-1 Related Classifications
HY-103084 Related Classifications
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