Rp-8-pCPT-Cyclic GMPS (sodium salt)
IC50: 18.3 and 0.16 μM for cGK Iα and cGK II, respectively.
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: Up to now, there is no animal in vivo study reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 525.9 |
Cas No. | 208445-07-2 |
Formula | C16H14ClN5O6PS2·Na |
Synonyms | Rp-8-pCPT-cGMPS |
Solubility | Soluble in H2O |
Chemical Name | 8-[(4-chlorophenyl)thio]-cyclic 3’,5’-[hydrogen [P(R)]-phosphorothioate] guanosine, monosodium salt |
SDF | Download SDF |
Canonical SMILES | O[C@H]1[C@H](N2C(SC3=CC=C(Cl)C=C3)=NC4=C2N=C(N)NC4=O)O[C@H]5[C@H]1O[P@@](OC5)([S-])=O.[Na+] |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
