8-CPT-Cyclic AMP (sodium salt) (Synonyms: 8-(p-Chlorophenylthio)-cAMP,8-CPT-cAMP) |
カタログ番号GC15352 |
8-CPT-Cyclic AMP (8-CPT-cAMP) ナトリウムは、サイクリック AMP 依存性プロテインキナーゼ (PKA) の選択的活性化因子です。
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Cas No.: 93882-12-3
Sample solution is provided at 25 µL, 10mM.
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).
Cas No. | 93882-12-3 | SDF | |
同義語 | 8-(p-Chlorophenylthio)-cAMP,8-CPT-cAMP | ||
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+] | ||
Formula | C16H14ClN5O6PS • Na | M.Wt | 493.8 |
溶解度 | ≤25mg/ml in Water | Storage | Store at -20°C |
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 | 2.0251 mL | 10.1256 mL | 20.2511 mL |
5 mM | 0.405 mL | 2.0251 mL | 4.0502 mL |
10 mM | 0.2025 mL | 1.0126 mL | 2.0251 mL |
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- Purity: >98.00%
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