OPC 3911
OPC 3911 is a highly selective inhibitor of cGMP-inhibited cAMP phosphodiesterase (cGI-PDE/PDE3) and a vasodilator, with an IC50 of 0.042 μM against rat cGI-PDE. OPC 3911 upregulates the expression of Osteopontin. OPC 3911 mediates vasodilation of arterial smooth muscle, induces vasodilatory responses in isolated rat arteriovenous tissues, and exhibits additive vasodilatory effects with Isoprenaline (HY-108353) and Forskolin (HY-15371). OPC 3911 can be used in studies related to congestive heart failure and insulin resistance.
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- CAS. Nr.: 76470-87-6
- Formel: C21H30N2O4
- Molecular Weight:374.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
PDE3 42 nM (IC50) |
In Vitro
OPC 3911 (up to 30 μM) induces concentration-dependent relaxation of coronary and renal arteries pre-contracted with 30 mM K+, with EC50 values of 1.4 μM and 0.87 μM, respectively; however, at the dose of 30 μM, it only induces 42% relaxation of pulmonary arteries pre-contracted with 30 mM K+[1].
OPC 3911 potently inhibits the cGMP-inhibited low Km cAMP phosphodiesterase purified from rat adipose tissue, with an IC50 of 0.042 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 76470-87-6
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Molecular Weight 374.48
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Formel C21H30N2O4
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SMILES
O=C1NC2=CC=C(OCCCC(=O)N(CCO)C3CCCCC3)C=C2CC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Lindgren S, et al. Effects of selective phosphodiesterase inhibitors on isolated coronary, lung and renal arteries from man and rat. Acta physiologica Scandinavica. 1991 May;142(1):77-82. [Content Brief]
[2]. Lindgren S, et al. Relaxant effects of the selective phosphodiesterase inhibitors milrinone and OPC 3911 on isolated human mesenteric vessels. Pharmacology & toxicology. 1989 May;64(5):440-5. [Content Brief]
[3]. Omar B, et al. Regulation of the pro-inflammatory cytokine osteopontin by GIP in adipocytes--a role for the transcription factor NFAT and phosphodiesterase 3B. Biochem Biophys Res Commun. 2012 Sep 7;425(4):812-7. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
OPC 3911 Related Classifications
HY-165568 Related Classifications
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