| Identification | Back Directory | [Name]
RP-8-BROMO-BETA-PHENYL-1,N2-ETHENOGUANOSINE 3',5'-CYCLIC MONOPHOSPHOROTHIOATE SODIUM SALT HYDRATE | [CAS]
185246-32-6 | [Synonyms]
Rp 8 Br PET cGMPS,Rp8BrPETcGMPS
Rp-8-bromo-PET-Cyclic GMPS sodium
Rp-8-bromo-PET-Cyclic GMPS (sodium salt)
Rp-8-Bromo-β-phenyl-1,N2-ethenoguanosine 3′,5′-cyclic monophosphorothioate
Rp-8-Bromo-beta-phenyl-1,N2-ethenoguanosine 3',5'-cyclic monophosphorothioate sodium salt
RP-8-BROMO-BETA-PHENYL-1,N2-ETHENOGUANOSINE 3',5'-CYCLIC MONOPHOSPHOROTHIOATE SODIUM SALT HYDRATE
Rp-8-Bromo-β-phenyl-1,N2-ethenoguanosine 3μ:5μ-cyclic monophosphorothioate hydrate sodium salt
Rp-8-Bromo-beta-phenyl-1,N2-ethenoguanosine 3',5'-cyclic monophosphorothioate sodium salt >=98% (HPLC), powder
Rp-8-Br-PET-cGMPS hydrate, Rp-β-Phenyl-1,N2-etheno-8-bromoguanosine 3μ,5μ-cyclic monophosphorothioate hydrate sodium salt | [Molecular Formula]
C18H14BrN5NaO6PS | [MOL File]
185246-32-6.mol | [Molecular Weight]
562.266 |
| Chemical Properties | Back Directory | [Melting point ]
240-300 °C(lit.) | [storage temp. ]
-20°C | [solubility ]
H2O: soluble15mg/mL at ≤60°C | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 15mg/mL at≤60°C |
| Hazard Information | Back Directory | [Description]
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis = 35 and 30 nM). It less potently inhibits protein kinase A (Ki = 11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50 = 25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki = 1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11. | [Uses]
Rp-8-Br-PET-cyclic GMPS Sodium Salt is a competitive inhibitor of cGMP-dependent protein kinase (cGKI). | [Biochem/physiol Actions]
Rp-8-Br-PET-cGMPS is metabolically stable, competitive inhibitor of cGMP-dependent protein kinase G. Inhibits both PKG I (Ki?=?30 nM) and PKG II and blocks cGMP-gated retinal type ion channels (IC50?=?25 micromoles). | [storage]
Store at -20°C | [References]
[1] E BUTT. Inhibition of cyclic GMP-dependent protein kinase-mediated effects by (Rp)-8-bromo-PET-cyclic GMPS.[J]. British Journal of Pharmacology, 1995, 116 8: 3110-3116. DOI: 10.1111/j.1476-5381.1995.tb15112.x
[2] NADEJDA VALTCHEVA. 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]. The Journal of Biological Chemistry, 2009, 284 1: 556-562. DOI: 10.1074/jbc.m806161200
[3] JI-YE WEI. Identification of Competitive Antagonists of the Rod Photoreceptor cGMP-Gated Cation Channel: β-Phenyl-1,N2-etheno-Substituted cGMP Analogues as Probes of the cGMP-Binding Site?[J]. Biochemistry Biochemistry, 1996, 35 51: 16815-16823. DOI: 10.1021/bi961763v
[4] RONALD J?GER. Activation of PDE10 and PDE11 phosphodiesterases.[J]. The Journal of Biological Chemistry, 2012: 1210-1219. DOI: 10.1074/jbc.m111.263806 |
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