CI-930
CI-930 is a selective, orally active phosphodiesterase 3 (PDE3) inhibitor with an IC50 value of 0.0.84 μM. CI-930 exerts positive inotropic and vasodilatory effects by inhibiting cAMP hydrolysis. CI-930 also regulates hemodynamics, inhibits the proliferation of coronary artery smooth muscle cells, and suppresses the proliferation of mouse splenocytes. CI-930 can be used in research related to heart failure, atherosclerosis, and asthma.
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- CAS 番号: 86798-59-6
- 分子式: C14H14N4O
- 分子量:254.29
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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PDE3 |
CI-930 (0.10-100.00 μM; 10 min) significantly inhibits soluble PDE activity in human coronary artery smooth muscle cells (HCASMCs), reaching a maximum inhibition rate of approximately 43% at concentrations of 10-100 μM[3].
PDE3, the PDE isoform inhibited by CI-930 (10 μM), is expressed in both soluble and particulate fractions of quiescent HCASMCs, accounting for 42%-44% of total PDE activity[3].
CI-930 (10 μM) inhibits PDE3, a PDE that is expressed in both the soluble and particulate fractions of proliferative HCASMCs, accounting for 44%-45% of total PDE activity[3].
CI-930 (10-20 μM; 24-30 h) inhibits the proliferation of human coronary artery smooth muscle cells (HCASMCs): at a concentration of 10 μM, the proportion of S-phase cells decreases significantly by 33%; at a concentration of 20 μM, the proportion of S-phase cells also decreases significantly[3].
CI-930 (20 μM; 15-25 h) alone does not induce a statistically significant increase in cAMP levels in HCASMCs[3].
CI-930 (10 μM; 6 h) does not affect the steady-state level of IL-2 mRNA in human Jurkat leukemia T cells activated by PHA/PMA[4].
CI-930 (1 nM-10 μM; 72 h) inhibits Concanavalin A (Con A, HY-P2149, 2.5 μg/mL)-induced proliferation of mouse splenocytes with an IC50 of 4.4 μM, and results from MTT-based cell viability assays demonstrate that the inhibitory effect on cells is not caused by cell death[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human coronary artery smooth muscle cells (HCASMC) from 32-year-old, 48-year-old, 58-year-old male donors, and a 61-year-old female donor
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Concentration:10 μM, 20 μM
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Incubation Time:24-30 h
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Result:Produced an 11-18% reduction in the percentage of cells in S phase across the three male donors, with a statistically significant reduction observed only in the 58-year-old male donor at 20 μM.
Produced a statistically significant 33% reduction in the percentage of cells in S phase in HCASMC from the 61-year-old female donor at 10 μM.
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Cell Line:human Jurkat leukemic T cells
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Concentration:10 μM
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Incubation Time:6 h
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Result:Showed unchanged steady-state levels of IL-2 mRNA in activated Jurkat cells, as confirmed by visualization of amplified PCR fragments and hybridization with a radiolabelled IL-2 probe.
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Cell Line:Concanavalin A-induced mouse splenocytes
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Concentration:10 μM, 1 μM, 0.1 μM, 30 nM, 1 nM
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Incubation Time:72 h
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Result:Inhibited concanavalin A-induced murine splenocyte proliferation with an IC50 of 4.4 μM.
MTT viability assay demonstrated that the antiproliferative effect was not due to cytotoxic cell death.
CI-930 (0.3-10 mg/kg; p.o.; twice daily) completely inhibits antigen-induced pulmonary eosinophilia and neutrophilia in Brown Norway rats, with ED50 values of 0.4 mg/kg and 0.5 mg/kg for twice-daily administration, respectively, showing comparable potency[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Brown Norway rats (male; 175-200 g at sensitization, 190-270 g at antigen challenge; allergic pulmonary inflammation model via ovalbumin sensitization and challenge with Bordetella pertussis adjuvant)[5]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; B.I.D.
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Result:Significantly inhibited antigen-induced eosinophil influx at 0.3-3 mg/kg.
Completely inhibited eosinophil influx at 10 mg/kg.
Achieved a B.I.D.
ED50 of 0.4 mg/kg for eosinophil influx inhibition.
Significantly inhibited antigen-induced neutrophil influx at 1-10 mg/kg.
Completely inhibited neutrophil influx at 10 mg/kg.
Achieved a B.I.D.
ED50 of 0.5 mg/kg for neutrophil influx inhibition.
化学情報
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CAS 番号 86798-59-6
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分子量 254.29
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分子式 C14H14N4O
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SMILES
O=C1NN=C(C(C1)C)C2=CC=C(N3C=NC=C3)C=C2
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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
[2]. Jafri SM, et al. Hemodynamic, Pharmacokinetic and Clinical Response to CI-930 in Congestive Heart Failure Due to Ischemic or Dilated Cardiomyopathy. The American Journal of Cardiology. 1987;59(11):1126-1130. [Content Brief]
[3]. Johnson-Mills K, et al. Effect of CI-930 [3-(2H)-pyridazinone-4,5-dihydro-6-[4-(1H-imidazolyl) phenyl]-5-methyl-monohydrochloride] and rolipram on human coronary artery smooth muscle cell proliferation. Biochemical pharmacology. 1998 Oct 15;56(8):1065-73. [Content Brief]
[4]. Lewis GM, et al. Effects of rolipram and CI-930 on IL-2 mRNA transcription in human Jurkat cells. Agents and actions. 1993;39 Spec No:C89-92. [Content Brief]
[5]. Howell RE, et al. Inhibition of antigen-induced pulmonary eosinophilia and neutrophilia by selective inhibitors of phosphodiesterase types 3 or 4 in Brown Norway rats. Pulmonary pharmacology. 1995;8(2-3):83-9. [Content Brief]
[6]. Gouault N et al. Solid-phase synthesis and evaluation of libraries of substituted 4,5-dihydropyridazinones as vasodilator agents. J Pharm Pharmacol. 2004 Aug;56(8):1029-37. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CI-930 関連分類
HY-183455 関連分類
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