| CAS NO: | 37762-06-4 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Cas No. | 37762-06-4 |
| 别名 | 2-(2-丙氧苯基)-8-氮杂次黄嘌呤,M&B 22948 |
| 化学名 | 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 |
| 分子式 | C13H13N5O2 |
| 分子量 | 271.28 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml |
| 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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