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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 76470-87-6
- 分子式: C21H30N2O4
- 分子量:374.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[2]|
PDE3 42 nM (IC50) |
体外実験
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.
化学情報
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CAS 番号 76470-87-6
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分子量 374.48
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分子式 C21H30N2O4
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SMILES
O=C1NC2=CC=C(OCCCC(=O)N(CCO)C3CCCCC3)C=C2CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)