An inhibitor of cGKI and cGKII
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Rp-8-bromo-PET-Cyclic GMPS (sodium salt)

Item No. 18823

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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, monosodium salt
CAS Number
185246-32-6
Synonyms
  • Rp-8-bromo-PET-cGMPS
Molecular Formula
C18H14BrN5O6PS • Na
Formula Weight
562.3
Purity
≥99%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Water: soluble
SMILES
O[C@H]1[C@H](N2C(Br)=NC3=C2NC4=NC(C5=CC=CC=C5)=CN4C3=O)O[C@@]6([H])[C@@]1([H])O[P@@](OC6)([S-])=O.[Na+]
InChi Code
InChI=1S/C18H15BrN5O6PS.Na/c19-17-21-11-14(24(17)16-12(25)13-10(29-16)7-28-31(27,32)30-13)22-18-20-9(6-23(18)15(11)26)8-4-2-1-3-5-8;/h1-6,10,12-13,16,25H,7H2,(H,20,22)(H,27,32);/q;+1/p-1/t10-,12-,13-,16-,31-;/m1./s1
InChi Key
SVMPQLHYWRTQCX-DBHVCDLJSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $294

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    Product 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).1,2 It less potently inhibits protein kinase A (Ki = 11 µM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50 = 25 µM).1,3 In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki = 1 µM).2 Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Butt, E., Pöhler, D., Genieser, H.G., et al. Inhibition of cyclic GMP-dependent protein kinase-mediated effects by (Rp)-8-bromo-PET-cyclic GMPS. Br. J. Pharmacol. 116(8), 3110-3116 (1995).

    2. Valtcheva, N., Nestorov, P., Beck, A., et al. 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. The Journal of Biological Chemisty 284(1), 556-562 (2009).

    3. Wei, J.Y., Cohen, E.D., Yan, Y.Y., et al. 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(51), 16815-16823 (1996).

    4. Jäger, R., Russwurm, C., Schwede, F., et al. Activation of PDE10 and PDE11 phosphodiesterases. The Journal of Biological Chemisty 287(2), 1210-1219 (2012).