6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE7-n-Butyl-6-(4-hydroxyphenyl)[5H]-pyrrolo[2,3-b]pyrazineRP-1074-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenolAloisine A RP107RP107, 7-n-Butyl-6-(4-hydroxyphenyl)-[5H]pyrrolo[2,3-b]pyrazine
Biochem/physiol Actions RP107 is an activator of cystic fibrosis transmembrane conductance regulator (CFTR) channel. RP107 stimulates wild-type CFTR and mutated CFTR with submicromolar affinity by a cAMP-independent mechanism. EC50 = 89 nM at activating CFTR-dependent C-secretion, an effect inhibited by CFTR(inh)-172 and glibenclaminde. RP107 constitutes a new example of a scaffold structure for the selective activation of CFTR receptors.
A cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks: IC50 =150nM, 120 nM, 400 nM and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25,