| 货号 | 18823-5mg |
| 描述 | 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 |
| 别名 | Rp-8-bromo-PET-cGMPS; |
| 供应商 | Cayman |
| 应用文献 | |
| 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. British Journal of Pharmacology 116, 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). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥99% |
| 计算分子量 | 562.3 |
| 分子式 | C18H14BrN5O6PS • Na |
| CAS号 | 185246-32-6 |
| 稳定性 | ≥ 2 years |
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