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PDE inhibitor
Potent, non-specific inhibitor of phosphodiesterases (IC50=2-50µM). More potent than theophylline at adenosine receptors. Accelerates conversion of mouse fibroblast cells into adipose cells.
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Product Details
| Appearance |
White solid. |
|---|---|
| CAS |
28822-58-4 |
| Couple Target |
PDE |
| Couple Type |
Inhibitor |
| Formula |
C10H14N4O2 |
| Identity |
Determined by NMR. |
| MW |
222.2 |
| Purity |
≥99% (HPLC) |
| RTECS |
ZD8500000 |
| Solubility |
Soluble in 100% ethanol, DMSO or methanol (warm, 50mg/ml); almost insoluble in water. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Store, as supplied at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Blue Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Adipocyte sphingosine kinase 1 regulates histone modifiers to disrupt circadian function: Anderson, A., Kovilakath, A., et al.; bioRxiv , (2024)
- PGE2-EP2/EP4 signaling elicits immunosuppression by driving the mregDC-Treg axis in inflammatory tumor microenvironment: D. Thumkeo, et al.; Cell Rep. 39, 110914 (2022), Abstract
- P-Rex1 Controls Sphingosine 1-Phosphate Receptor Signalling, Morphology, and Cell-Cycle Progression in Neuronal Cells: Hampson, E., Tsonou, E., et al.; Cells 10, (2021), Abstract
- Exendin-4 stimulates autophagy in pancreatic β-cells via the RAPGEF/EPAC-Ca2+-PPP3/calcineurin-TFEB axis: F.P. Zummo, et al.; Autophagy , (2021), Abstract
- Loss of Slc26a9 anion transporter alters intestinal electrolyte and HCO3(-) transport and reduces survival in CFTR-deficient mice: Liu, X., Li, T., et al.; Pflugers Arch. 467, 1261 (2015), Abstract
- Adrenergic and serotonin receptors affect retinal superoxide generation in diabetic mice: relationship to capillary degeneration and permeability: Du, Y., Cramer, M., et al.; FASEB J. 29, 2194 (2015), Abstract
- Crosstalk between PKA and Epac regulates the phenotypic maturation and function of human dendritic cells: Garay, J., D’Angelo, J. A., et al.; J. Immunol. 185, 3227 (2010), Abstract
- Effect of an antihypertensive hydrazine derivative on Ca2+ current of single frog cardiac cells: F. Scamps, et al.; Eur. J. Pharmacol. 244, 119 (1993), Abstract
- Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity: C. Tomes, et al.; Cell. Signal. 5, 615 (1993), Abstract
- Bemoradan–a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue: J.B. Moore, Jr., et al.; Biochem. Pharmacol. 42, 679 (1991), Abstract
- Differential effects of Ro 20-1724 and isobutylmethylxanthine on the basal force of contraction and beta-adrenoceptor-mediated response in the rat ventricular myocardium: Y. Katano & M. Endoh; BBRC 167, 123 (1990), Abstract
- Psychomotor-stimulant effects of 3-isobutyl-1-methylxanthine: comparison with caffeine and 7-(2-chloroethyl) theophylline: V.L. Coffin and R.D. Spealman; Eur. J. Pharmacol. 170, 35 (1989), Abstract
- Methylxanthine inhibitors of phosphodiesterases: J.N. Wells & J.R. Miller; Methods Enzymol. 159, 489 (1988), Abstract
- Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes: R.F. Bruns, et al.; Mol. Pharmacol. 29, 331 (1986), Abstract
- Selective inhibition of cyclic AMP and cyclic GMP phosphodiesterases of cardiac nuclear fraction: G.S. Ahluwalia & A.R. Rhoads; Biochem. Pharmacol. 31, 665 (1982), Abstract
- Inhibition of growth of primary and metastatic Lewis lung carcinoma cells by the phosphodiesterase inhibitor isobutylmethylxanthine: P. Janik, et al.; Cancer Res. 40, 1950 (1980), Abstract
- Induction of a transient elevation in intracellular levels of adenosine-3’,5’-cyclic monophosphate by chemotactic factors: an early event in human neutrophil activation: L. Simchowitz, et al.; J. Immunol. 124, 1482 (1980), Abstract
- Differentiation of 3T3-L2 fibroblasts into adipose cells in bromodeoxyuridine-suppressed cultures: T.R. Russell; PNAS 76, 4451 (1979), Abstract
- Selective inhibition of cyclic nucleotide phosphodiesterases by analogues of 1-methyl-3-isobutylxanthine: G.L. Kramer, et al.; Biochemistry 16, 3316 (1977), Abstract
- Methyl xanthine phosphodiesterase inhibitors behave as prostaglandin antagonists in a perfused rat mesenteric artery preparation: D.F. Horrobin, et al.; Prostaglandins 13, 33 (1977), Abstract
- Cyclic nucleotide phosphodiesterases of human and rat gastric mucosa: U. Klotz, et al.; Naunyn-Schmiedebergs Arch. Pharmacol. 296, 187 (1977), Abstract
- Allergic reactions, cyclic AMP and histamine release: P.S. Skov, et al.; Experientia 33, 965 (1977), Abstract
- Determination of theophylline in plasma by electron capture gas chromatography: H.A. Schwertner, et al.; Anal. Chem. 48, 1875 (1976), Abstract
- The mode of action of adenosine 3’:5’-cyclic monophosphate in mammalian islets of Langerhans. Effects of insulin secretagogues on islet-cell protein kinase activity: W. Montague & S.L. Howell; Biochem. J. 134, 321 (1973), Abstract
- Concentration of adenosine 3’:5’-cyclic monophosphate in mouse pancreatic islets measured by a protein-binding radioassay: R.H. Cooper, et al.; Biochem. J. 134, 599 (1973), Abstract
- Effects of methylxanthines on adenosine 3’,5’-monophosphate and corticosterone in the rat adrenal: A. Peytremann, et al.; Endocrinology 92, 525 (1973), Abstract
- Cyclic nucleotide phosphodiesterase activity in normal mouse pancreatic islets: S.J. Ashcroft, et al.; FEBS Lett. 20, 263 (1972), Abstract
- The role of adenosine 3′:5′-cyclic monophosphate in the regulation of insulin release by isolated rat islets of Langerhans: W. Montague & J.R. Cook; Biochem. J. 122, 115 (1971), Abstract
- Adenosine 3′:5′-cyclic monophosphate and insulin release: W. Montague & J.R. Cook; Biochem. J. 120, 9P (1970), Abstract
- Effects of xanthine derivatives on lipolysis and on adenosine 3′,5′- monophosphate phosphodiesterase activity: J.A. Beavo, et al.; Mol. Pharmacol. 6, 597 (1970), Abstract
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