| Identification | Back Directory | [Name]
Rp-8-pCPT-Cyclic GMPS (sodium salt) | [CAS]
208445-07-2 | [Synonyms]
Rp-8-pCPT-cGMPS sodium
Rp-8-pCPT-Cyclic GMPS (sodium salt)
8-[(4-Chlorophenyl)thio]-guanosine-cyclic 3',5'-[hydrogen [P(R)]-phosphorothioate] sodium | [Molecular Formula]
C16H14ClN5NaO6PS2 | [MOL File]
208445-07-2.mol | [Molecular Weight]
525.859 |
| Hazard Information | Back Directory | [Uses]
Rp-8-pCPT-Cyclic GMPS Sodium Salt acts as a stable cell-permeable analog which competetively inhibits cGMP-dependant protein kinases affecting the nervous system. | [Biological Activity]
rp-8-pcpt-cyclic gmps is a gmp-dependent protein kinases (cgks) inhibitor.appreciation of cgmp as a distinct intracellular second messenger is reported to be closely followed by an intensive search for effector proteins in various organisms. a cgmp-dependent protein kinase (cgk) has been found in arthropods resulting in the eventual isolation of cgk from mammalian tissues. | [in vitro]
previous study found that rp-8-pcpt-cyclic gmps could selectively inhibit cgk activity in intact human platelets. the ic50 value of rp-8-pcpt-cyclic gmps for cgk ii was 114-fold lower than that for cgk iα in the presence of 1 mm cgmp. in the presence of 10 mm cgmp, the ic50 values of rp-8-pcpt-cyclic gmps for cgk iα and cgk ii increased 3- and 11-fold, respectively. in addition, millimolar concentrations of rp-8-pcpt-cyclic gmps could fully activate both enzymes, a phenomenon that was observed previously for cgk ii. because substitutions at the 8-position of the guanine ring are poorly tolerated by cgk ib, these results suggested that the rp-isomer of 8-pcpt-cgmps might be a selective activator or inhibitor, respectively, of cgk ii compared to the cgk i isoforms [1]. | [in vivo]
Rp-8-pCPT-cGMPS sodium (5 nM, intrathecally, once a day for 3 days) inhibits the cGMP-cGKI pathway, suppresses tumor cell implantation (TCI)-induced thermal hyperalgesia and mechanical allodynia in Sprague-Dawley rats model[1]. | Animal Model: | Bone cancer pain induced by tumor cell implantation (TCI) in Sprague-Dawley rats[1]. | | Dosage: | 0.5 mmol/L, 20 μL | | Administration: | intrathecally, once a day for 3 days | | Result: | Delayed and suppressed TCI-induced thermal hyperalgesia and mechanical allodynia. |
| [IC 50]
18.3 and 0.16 μm for cgk iα and cgk ii, respectively. | [storage]
Store at -20°C | [References]
[1] gamm, d. m.,francis, s.h.,angelotti, t.p., et al. the type ii isoform of cgmp-dependent protein kinase is dimeric and possesses regulatory and catalytic properties distinct from the type i isoforms. the journal of biological chemisty 270(45), 27380-27388 (1995). |
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