country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-103084

Copy Link Print Information

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2109805-65-2
Formel: C₂₂H₁₄N₂O₄S
Molecular Weight:402.42

Speicherung:

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

PDE5-IN-1 Chemical Structure

CAS. Nr.: 2109805-65-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

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

Species	Dose	Route	T_1/2	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	T_max	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	/	/

In Vivo

PDE5-IN-1 (compound 2) (5.0 mg/kg; p.o.; daily; 3 weeks) produces a statistically significant reduction in mPAP and RVHI in MCT-induced PAH rats^[1].

MedChemExpress (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.

Chemical Information

CAS. Nr. 2109805-65-2
Molecular Weight 402.42
Formel C₂₂H₁₄N₂O₄S
SMILES

O=C1C=2C=CC=CC2OC=3C1=C(NC3CC4=CC=C5OCOC5=C4)C6=NC=CS6
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wu D,et al. Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2017 Aug 10;60(15):6622-6637. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen