Etazolate hydrochloridePDE4 inhibitor CAS# 35838-58-5 |
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Quality Control & MSDS
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| Cas No. | 35838-58-5 | SDF | Download SDF |
| PubChem ID | 37274 | Appearance | Powder |
| Formula | C14H20ClN5O2 | M.Wt | 325.8 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in water and to 100 mM in DMSO | ||
| Chemical Name | ethyl 1-ethyl-4-(2-propan-2-ylidenehydrazinyl)pyrazolo[3,4-b]pyridine-5-carboxylate;hydrochloride | ||
| SMILES | CCN1C2=NC=C(C(=C2C=N1)NN=C(C)C)C(=O)OCC.Cl | ||
| Standard InChIKey | GQJUGJHJUZSJLZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H19N5O2.ClH/c1-5-19-13-10(8-16-19)12(18-17-9(3)4)11(7-15-13)14(20)21-6-2;/h7-8H,5-6H2,1-4H3,(H,15,18);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Phosphodiesterase inhibitor, selective for PDE4 (IC50 = 2.0 μM). |
Etazolate hydrochloride Dilution Calculator
Etazolate hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0694 mL | 15.3468 mL | 30.6937 mL | 61.3874 mL | 76.7342 mL |
| 5 mM | 0.6139 mL | 3.0694 mL | 6.1387 mL | 12.2775 mL | 15.3468 mL |
| 10 mM | 0.3069 mL | 1.5347 mL | 3.0694 mL | 6.1387 mL | 7.6734 mL |
| 50 mM | 0.0614 mL | 0.3069 mL | 0.6139 mL | 1.2277 mL | 1.5347 mL |
| 100 mM | 0.0307 mL | 0.1535 mL | 0.3069 mL | 0.6139 mL | 0.7673 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Hydrolysis and subsequent cyclization of etazolate hydrochloride and related compounds in aqueous solutions: application of PMR and mass spectrometry in accelerated stability studies.[Pubmed:660474]
J Pharm Sci. 1978 Jun;67(6):850-3.
The hydrolysis of Etazolate hydrochloride, an inhibitor of cyclic nucleotide 3',5'-monophosphate phosphodiesterase that degrades cyclic adenosine 3',5'-monophosphate (cyclic AMP) to adenosine 5'-monophosphate, and related compounds was studied by PMR and mass spectrometry. The compounds underwent reversible acid-catalyzed hydrolysis in aqueous solutions at 60 degrees, followed by cyclization to a major and a minor product formed by independent pathways. Under the experimental conditions, the minor product was stable. The formation rate of the major product, 6-ethyl-1,6-dihydrodipyrazolo [3,4-b:3',4'-d] pyridin-3(2H)-one, was considerably greater than that of the minor component, 3-ethoxy-6-ethyl-1,6-dihydrodipyrazolo [3,4-b:3',4'-d] pyridine. For the 6-methyl analog of etazolate, the rate of methyl deuteration was considerably slower than the rate of cyclization.
Differential modulation of tissue function and therapeutic potential of selective inhibitors of cyclic nucleotide phosphodiesterase isoenzymes.[Pubmed:1848733]
Trends Pharmacol Sci. 1991 Jan;12(1):19-27.
Since the discovery of cyclic nucleotide phosphodiesterase 30 years ago, there have been major advances in our knowledge of this group of isoenzymes. Five families, each composed of several isoforms and having differing tissue distributions, have been described. David Nicholson and colleagues compare the tissue distribution of phosphodiesterase isoenzymes and discuss the differential effects of inhibition of particular isoenzymes, with differing subcellular localization, on tissue function. They also review the potential use of isoenzyme selective phosphodiesterase inhibitors in a range of clinical disorders such as heart failure, asthma, depression and dementia.
Selective inhibition of cyclic AMP and cyclic GMP phosphodiesterases of cardiac nuclear fraction.[Pubmed:6177320]
Biochem Pharmacol. 1982 Mar 1;31(5):665-9.
Approximately 60% of the total particulate phosphodiesterase activity occurring in cardiac tissue was associated with the nuclear fraction. Cyclic GMP phosphodiesterase activity of the purified cardiac nuclear fraction was selectively inhibited by trifluoperazine (I50 = 19 microM) with negligible inhibition (less than 15%) of cyclic AMP phosphodiesterase activity. Inhibition of cyclic GMP phosphodiesterase by trifluoperazine was calcium-dependent and suppressed by ethylene glycol bis (beta-aminoethyl ether)N, N, N', N'-tetraacetic acid (EGTA). The inhibitory response of both phosphodiesterases to papaverine was similar in the presence of calcium. However, in the presence of EGTA, papaverine inhibition of cyclic GMP but not cyclic AMP phosphodiesterase was reduced significantly. Calmodulin (1-5 micrograms/ml) readily reversed the inhibition by 25 microM trifluoperazine of membraneous cyclic GMP phosphodiesterase, but had no effect on inhibition by papaverine. With imidazolidinone analogues (Ro 7-2956 and Ro 20-1724), EGTA enhanced the inhibition of cyclic GMP phosphodiesterase without significantly altering the inhibition of cyclic AMP phosphodiesterase. Inhibition of cyclic AMP of cyclic GMP phosphodiesterase activity by 1-methyl-3-isobutylxanthine, quinidine, or compound SQ 20,009 was not affected appreciably by calcium or EGTA. The selective inhibitory action of certain pharmacological agents on phosphodiesterases of cardiac nuclear fraction and the modulation of the inhibitory response by calcium suggest an intrinsic and predominant association of calmodulin with cyclic GMP phosphodiesterase activity of these membranes.
