Rp-8-Br-PET-环状GMPS，钠盐是代谢稳定的竞争性cGKI抑制剂（cGKIα和β）。该化合物阻断cGMP门控的视网膜离子通道（IC | 50 | = 25μM）和纯化的II型PKA的活化（K | i | = 10μM）。Rp-8-Br-PET-环状GMPS，与Rp-8-pCPT-cGMPS相比，钠盐更具亲脂性和细胞渗透性。注意：1μmol= 0.56 mg。Rp-8-Br-PET-环状GMPS，钠盐是cGKII的抑制剂。
Rp-8-Br-PET-cyclic GMPS, Sodium Salt is a metabolically-stable, competitive inhibitor of cGKI (cGKI α and β). This compound blocks cGMP-gated retinal type ion channels (IC|50|= 25 μM) and the activation of purified PKA type II (K|i|= 10 μM). Rp-8-Br-PET-cyclic GMPS, Sodium Salt is more lipophilic and cell-permeable than Rp-8-pCPT-cGMPS . Note: 1 μmol = 0.56 mg. Rp-8-Br-PET-cyclic GMPS, Sodium Salt is an inhibitor of cGKII.
CAS编号：172806-20-1
熔点：240-300° C (lit.)
溶解性：Soluble in water (15 mg/ml at 60° C), and DMSO (40 mM).
储存温度：-20°C储存
分子量：562.3
分子式：C₁₈H₁₄BrN₅O₆PS・Na

Smiles
C1[C@@H]2[C@H]([C@H]([C@@H](O2)N3C4=C(C(=O)N5C=C(NC5=N4)C6=CC=CC=C6)N=C3Br)O)OP(=S)(O1)[O-].[Na+]
IC50
cGMP-gated retinal type ion channels: IC₅₀= 25 μM; PKA2: IC₅₀= 10 μM
PubChem CID：44755141

Ki Data
protein kinase G types 1α: Ki= 30 nM; protein kinase G types 1β: Ki= 30 nM; PKA2: Ki= 10 μM