| CAS NO: | 208445-07-2 |
| 包装: | 1mg |
| 市场价: | 3472元 |
| Cas No. | 208445-07-2 |
| 别名 | Rp-8-pCPT-cGMPS |
| 化学名 | 8-[(4-chlorophenyl)thio]-cyclic 3’,5’-[hydrogen [P(R)]-phosphorothioate] guanosine, monosodium salt |
| 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+] |
| 分子式 | C16H14ClN5O6PS2o Na |
| 分子量 | 525.9 |
| 溶解度 | Soluble in Water |
| 储存条件 | Store at -20℃ |
| 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: 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: |
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