CAS NO: | 93882-12-3 |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 493.8 |
Cas No. | 93882-12-3 |
Formula | C16H14ClN5O6PS·Na |
Synonyms | 8-(p-Chlorophenylthio)-cAMP,8-CPT-cAMP |
Solubility | ≤25mg/ml in H2O |
Chemical Name | 8-[(4-chlorophenyl)thio]-cyclic 3',5'-(hydrogen phosphate)-adenosine, monosodium salt |
Canonical SMILES | O[C@H]1[C@H](N2C(SC3=CC=C(Cl)C=C3)=NC4=C2N=CN=C4N)O[C@H]5[C@H]1OP(OC5)([O-])=O.[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Ka : 0.05 and 0.11 μM for PKA and PKG, respectively
8-CPT-Cyclic AMP is a lipophilic activator of the cyclic-AMP- and cyclic-GMP-dependent protein kinases, PKA and PKG.
The ability of cGMP-dependent protein kinases (cGKs) to activate cAMP response element (CRE)-dependent gene transcription was compared with that of cAMP-dependent protein kinases (cAKs).
In vitro: A previous study found that 8-CPT-Cyclic AMP was a potent activator of cAMP-PK and cyclic-GMP-dependent protein kinase (cGMP-PK) both as purified enzymes and in platelet membranes. 8-CPT-Cyclic AMP was hydrolysed to a significant extent by the Ca2+/calmodulin-dependent phosphodiesterase and by the cGMP-inhibited phosphodiesterase. Moreover, Sp-5,6- DCl-cBiMPS was also more effective than 8-CPT-Cyclic AMP in inducing quantitative phosphorylation of vasodilator-stimulated phosphoprotein in intact platelets [1]. Another study indicated that 8-CPT-Cyclic AMP was a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA). Indeed, 8-CPT-Cyclic AMP could inhibit PDE VA with a potency similar to that of zaprinast. In addition, 8-CPT-Cyclic AMP was metabolized by PDE VA at a rate half that of cyclic GMP. The cyclic GMP-inhibited phosphodiesterase and the cyclic AMP-specific phosphodiesterase could be inhibited by 8-CPT-Cyclic AMP as well [2].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Sandberg, M. ,Butt, E.,Nolte, C., et al. Characterization of Sp-5,6-dichloro-1-β-D-ribofuranosylbenzimidazole-3',5'-monophosphorothioate (Sp-5,6-DCl-cBiMPS) as a potent and specific activator of cyclic-AMP-dependent protein kinase in cell extracts and intact cells. Biochemistry Journal 279, 521-527 (1991).
[2] Connolly, B. J.,Willits, P.B.,Warrington, B.H., et al. 8-(4-chlorophenyl)thio-cyclic AMP is a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA). Biochemical Pharmacology 44(12), 2303-2306 (1992).