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.
For research use only. We do not sell to patients.
- CAS No.: 86798-59-6
- Formula: C14H14N4O
- Molecular Weight:254.29
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[5]|
PDE3 |
In Vitro
CI-930 (10 μM) inhibits PDE3, a PDE that is expressed in both the soluble and particulate fractions of proliferative HCASMC derived from 32-year-old and 58-year-old male donors, accounting for 44%-45% of total PDE activity[3].
CI-930 (20 μM; 15-25 h) alone does not induce a statistically significant increase in cAMP levels in HCASMC derived from male donors aged 32, 48, or 58 years[3].
PDE3, the PDE isoform inhibited by CI-930 (10 μM), is expressed in both soluble and particulate fractions of quiescent HCASMC derived from 48-year-old and 58-year-old male donors, accounting for 42%-44% of total PDE activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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
-
Concentration:10 μM, 20 μM
-
Incubation Time:24-30 h
-
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.
-
Cell Line:human Jurkat leukemic T cells
-
Concentration:10 μM
-
Incubation Time:6 h
-
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.
-
Cell Line:Concanavalin A-induced mouse splenocytes
-
Concentration:10 μM, 1 μM, 0.1 μM, 30 nM, 1 nM
-
Incubation Time:72 h
-
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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]
-
Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
-
Administration:p.o.; B.I.D.
-
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.
Chemical Information
-
CAS No. 86798-59-6
-
Molecular Weight 254.29
-
Formula C14H14N4O
-
SMILES
O=C1NN=C(C(C1)C)C2=CC=C(N3C=NC=C3)C=C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CI-930 Related Classifications
HY-183455 Related Classifications
Powered by Bioz