RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of receptor interacting serine/threonine kinase 1
Product Description
Information
RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Targets
RIP1 (Cell-free) 13 nM
In vitro
RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM. It showed no inhibition of RIP3 kinase activity at a 10 µM concentration. RIPA-56 does not inhibit IDO activity at a concentration of 200 µM, which represents an estimated 10,000-fold selectivity window based on the RIP1 ADP-Glo activity of 13 nM.
In vivo
RIPA-56 has an impressive PK profile in mice, with a 3.1 h half-life, 22% oral bioavailability (PO), and 100% bioavailability from intraperitoneal injection (IP). RIPA-56 has great ability in transporting across blood brain barrier. In the SIRS mice disease model, RIPA-56 efficiently reduced tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage.
This compound belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.