Rp-8-pCPT-Cyclic GMPS (sodium salt) (Synonyms: Rp-8-pCPT-cGMPS) |
| Catalog No.GC10706 |
GMP-dependent protein kinases (cGKs) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 208445-07-2
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 208445-07-2 | SDF | |
| Synonyms | Rp-8-pCPT-cGMPS | ||
| Chemical Name | 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+] | ||
| Formula | C16H14ClN5O6PS2 • Na | M.Wt | 525.9 |
| Solubility | Soluble 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9015 mL | 9.5075 mL | 19.015 mL |
| 5 mM | 0.3803 mL | 1.9015 mL | 3.803 mL |
| 10 mM | 0.1902 mL | 0.9508 mL | 1.9015 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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