Rp-8-bromo-Cyclic GMPS (sodium salt) (Synonyms: Rp-8-bromo-cGMPS) |
| Catalog No.GC10517 |
cGMP-dependent protein kinase (cGK) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 208445-06-1
Sample solution is provided at 25 µL, 10mM.
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Rp-8-bromo-Cyclic GMPS is a cGMP-dependent protein kinase (cGK) inhibitor.
cGMP is considered as an important regulator of vascular smooth muscle tone. Several smooth muscle relaxants including nitrogen oxide-containing vasodilators), endothelial-derived relaxing factors, and atrial natriuretic peptides can stimulate cGMP production in vascular smooth muscle. In addition, many of these agents have been shown to inhibit Ca2+-stimulated enzymes such as phosphorylase kinase and myosin light chain kinase in aortic smooth muscle, indicating that one major role of cGMP is to reduce the levels of free intracellular Ca2+.
In vitro: The effects of Rp-8-bromo-Cyclic GMPS on intracellular calcium concentrations in cultured rat aortic smooth muscle cells were studied. Results showed that both angiotensin II and depolarizing concentrations of K+ were ableo to stimulate Ca2+' accumulation in the cytoplasm. The increase in Ca2+ because of angiotensin II was associated with an increase in inositol phosphates, while that due to K+ was not. Preincubation of cells with Rp-8-bromo-Cyclic GMPS at 100 μM could cause an inhibition of peak Ca2+ accumulation to either angiotensin II or K+ [1]. Another study found that like 8-bromo-cGMP, Rp-8-bromo-Cyclic GMPS was also resistant to hydrolysis by phosphodiesterases. This Rp isomer could bind cGK without activating it, leading to the competitive inhibition [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] Rashatwar, S. S.,Cornwell, T.L. and Lincoln, T.M. Effects of 8-bromo-cGMP on Ca2+ levels in vascular smooth muscle cells: Possible regulation of Ca2+-ATPase by cGMP-dependent protein kinase. Proceedings of the National Academy of Sciences of the United States of America 84(16), 5685-5689 (1987).
[2] Butt, E. ,Phler, D.,Genieser, H.G., et al. Inhibition of cyclic GMP-dependent protein kinase-mediated effects by (Rp)-8-bromo-PET-cyclic GMPS. British Journal of Pharmacology 116, 3110-3116 (1995).
| Cas No. | 208445-06-1 | SDF | |
| Synonyms | Rp-8-bromo-cGMPS | ||
| Chemical Name | 8-bromo-guanosine cyclic 3',5'-[(R)-(hydrogen phosphorothioate)], monosodium salt | ||
| Canonical SMILES | O[C@H]1[C@H](N2C(Br)=NC3=C2N=C(N)NC3=O)O[C@H]4[C@H]1O[P@@](OC4)([S-])=O.[Na+] | ||
| Formula | C10H10BrN5O6PS • Na | M.Wt | 462.1 |
| Solubility | ≤3.6mg/ml in ethanol;12.5mg/ml in DMSO;16.7mg/ml in dimethyl formamide | 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 | 2.164 mL | 10.8202 mL | 21.6403 mL |
| 5 mM | 0.4328 mL | 2.164 mL | 4.3281 mL |
| 10 mM | 0.2164 mL | 1.082 mL | 2.164 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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