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Submit ReviewRp-8-Br-PET-cGMPS
Description: Protein kinase G inhibitor
Chemical Name: 2-Bromo-3,4-dihydro-3-[3,5-O-[(R)-mercaptophosphinylidene]-β-D-ribofuranosyl]-6-phenyl-9H-Imidazo[1,2-a]purin-9-one sodium salt
Purity: ≥99% (HPLC)
Biological Activity
Competitive, reversible cGMP-dependent protein kinase (PKG) inhibitor; cGMP analog.
This product is sold in units of 560μg, equivalent to 1μmol.
Technical Data
| M. Wt | 562.27 |
| Formula | C18H14BrN5NaO6PS |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 185246-32-6 |
| PubChem ID | 23695925 |
| InChI Key | PNUXBFRWMZKKAJ-IPZAVTHYSA-M |
| Smiles | [H][C@@]([C@@](O[C@@H](N3C(Br)=NC5=C3NC4=NC(C6=CC=CC=C6)=CN4C5=O)[C@@H]2O)([H])CO1)2O[P@@]1(S[Na])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 11.25 | 20 | |
| DMSO | 22.49 | 40 |
Preparing Stock Solutions
The following data is based on the product molecular weight 562.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 4.45 mL | 22.23 mL | 44.46 mL |
| 2 mM | 0.89 mL | 4.45 mL | 8.89 mL |
| 4 mM | 0.44 mL | 2.22 mL | 4.45 mL |
| 20 mM | 0.09 mL | 0.44 mL | 0.89 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Wei et al (1996) Identification of competitive antagonists of the rod photoreceptor cGMP-gated cation channel: beta-phenyl-1,N2-etheno-substituted cGMP analogues as probes of the cGMP-binding site. Biochemistry 35 16815 PMID: 8988020
Qi et al (2007) Protein kinase G regulates the basal tension and plays a major role in nitrovasodilator-induced relaxation of porcine coronary veins. Br.J.Pharmacol. 152 1060 PMID: 17891157
Valtcheva et al (2008) The commonly used cGMP-dependent protein kinase type I (cGKI) inhibitor Rp-8-Br-PET-cGMPS can activate cGKI in vitro and in intact cells. J.Biol.Chem. 284 556 PMID: 19008225
If you know of a relevant reference for Rp-8-Br-PET-cGMPS, please let us know.
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Keywords: Rp-8-Br-PET-cGMPS, Rp-8-Br-PET-cGMPS supplier, Protein, kinase, G, inhibitors, inhibits, PKG, Kinases, cGMP-dependent, Kinase, 3028, Tocris Bioscience
2 Citations for Rp-8-Br-PET-cGMPS
Citations are publications that use Tocris products. Selected citations for Rp-8-Br-PET-cGMPS include:
Berlinguer-Palmini et al (2013) GPR35 activation reduces Ca2+ transients and contributes to the kynurenic acid-dependent reduction of synaptic activity at CA3-CA1 synapses. PLoS One 8 e82180 PMID: 24312407
Lin et al (2008) Integrin regulation of cytoplasmic calcium in excitatory neurons depends upon glutamate receptors and release from intracellular stores. Cell 37 770 PMID: 18289871
Do you know of a great paper that uses Rp-8-Br-PET-cGMPS from Tocris? Please let us know.
Reviews for Rp-8-Br-PET-cGMPS
Average Rating: 5 (Based on 1 Review.)
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Filter by:
PKG inhibitor in vitro.
By
Anonymous on 08/11/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Neuron
Used in cultured neurons at 10 uM
Excellent PKG inhibitor
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