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Drug intelligence / Profile preview
Rp-8-Br-cAMPS-pAB
- Development stage
- Unknown
- Lead developer
- BIOLOG Life Science Institute
- Modality
- Small Molecules
01
Overview
Rp-8-Br-cAMPS-pAB (Rp-pAB) is a highly membrane-permeable, bioactivatable para-acetoxybenzyl (pAB) ester prodrug of the cyclic adenosine monophosphate (cAMP) antagonist Rp-8-Br-cAMPS. Developed as a pharmacological research tool, it is metabolized by ubiquitous cytosolic esterases to release the active free Rp-8-Br-cAMPS. Once bioactivated, it acts as a dual competitive antagonist of both protein kinase A (PKA) and exchange proteins directly activated by cAMP (Epac1 and Epac2). Rp-8-Br-cAMPS-pAB is widely used in laboratory research to investigate cAMP-dependent signaling pathways, particularly in pancreatic beta-cells where it has been shown to selectively inhibit first-phase glucose-stimulated insulin secretion (GSIS) and block GLP-1 receptor-mediated signaling.
- Other names
- 8-bromoadenosine-3',5'-cyclic monophosphorothioate, Rp-isomer, 4-acetoxybenzyl esterRp-8-Br-cAMPS-pABRp8-Br-cAMPS-pABRp 8-Br-cAMPS-pABRp-pAB
02
Targets
EPAC1 (Rap guanine nucleotide exchange factor 3)EPAC2 (Rap guanine nucleotide exchange factor 4)PKA (Cyclic amp-dependent protein kinase)
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