Zaprinast (Synonyms: 2(oPropoxyphenyl)8azapurin6one, M&B 22,948) |
| Katalog-Nr.GC12909 |
Zaprinast (M&B 22948) ist ein Inhibitor cGMP-selektiver Phosphodiesterasen (PDEs).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 37762-06-4
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.15, 0.76, 12.0 and 29.0 μM for PDE6, 5, 11 and 9 respectively.
Zaprinast is a phosphodiesterase inhibitor with selection for PDE6, 5, 11 and 9[1].
Several isoforms of phosphodiesterases (PDEs) can mediate their action of the diverse cellular and behavioral responses to these second messengers. Accordingly, these responses are modulated by the rates of synthesis of cyclic nucleotides by cyclases as well as their degradation by PDEs to biologically inactive 59 monophosphate nucleosides.
In vitro: Zaprinast is a PDE5 and PDE6 inhibitor with inhibiting PDE9 at moderately high concentrations (29 mM) [1]. Indeed, it showed that inhibition of cGMP hydrolysis by infusion of zaprinast increases the effect of ANP on natriuresis with no causing deleterious drops in blood pressure. Because it was known that ANP receptors is localized within the glomerulus and inner medullary collecting ducts, to determine the cellular localization of PDE9 enzyme in kidney will be interesting. [2]. The enzyme displayed a high specificity for cGMP with binding sites for cGMP, and a sensitivity to zaprinast similar to smooth muscle PDE5, resulting in both enzymes were named cGMP-PDE. However, retinal cGMP-PDE was first distinguished as photoreceptor cGMP-PDE with being specifically distributed in the retina and having a higher Vmax and Km values than other cGMP-PDEs and being modulated by G protein. [3].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Christensen and Torphy (1994) Isozyme-selective phosphodiesterase inhibitors as antiasthmatic agents. Annu.Rep.Med.Chem. 29 185.
[2] Soderling SH, Bayuga SJ, Beavo JA. Identification and characterization of a novel family of cyclic nucleotide phosphodiesterases. J Biol Chem. 1998 Jun 19; 273(25):15553-8.
[3]. Lugnier C. Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific therapeutic agents. Pharmacol Ther. 2006 Mar; 109 (3):366-98. Epub 2005 Aug 15.
| Cas No. | 37762-06-4 | SDF | |
| Überlieferungen | 2(oPropoxyphenyl)8azapurin6one, M&B 22,948 | ||
| Chemical Name | 5-(2-propoxyphenyl)-2H-[1,2,3]triazolo[4,5-d]pyrimidin-7(3H)-one | ||
| Canonical SMILES | O=C1N=C(C2=CC=CC=C2OCCC)N=C3NNN=C31 | ||
| Formula | C13H13N5O2 | M.Wt | 271.28 |
| Löslichkeit | DMF: 20 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6862 mL | 18.4311 mL | 36.8623 mL |
| 5 mM | 0.7372 mL | 3.6862 mL | 7.3725 mL |
| 10 mM | 0.3686 mL | 1.8431 mL | 3.6862 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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