A cell-permeable, dimeric pentapeptide (IETDV) derived from GluN2B C-terminal and linked through a polyethylene glycol (PEG)-based linker that inhibits the ternary protein complex of PSD-95 (postsynaptic density protein-95), nNOS, and NMDA by directly binding to the tandem PDZ1 and 2 domains of PSD-95 (Ki = 4.6 nM). This inhibition results in the uncoupling between NMDA receptor activity and nitric oxide production without affecting NMDA-mediated ion channel gating function and pro-survival signaling pathways. Exhibits about 1000-fold higher potency than the monomeric Tat-NR2B9c. Exhibits improved plasma stability, with t1/2 ~ 80 hours. Shown to cross the blood-brain barrier and reduce infarct volume by about 40% and restore motor functions in mice subjected to focal ischemic brain damage.
Biochem/physiol Actions
Cell permeable: yes
Primary Target PSD95
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
Supplied as a trifluoroacetate salt.
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bach, A., et al. 2012. Proc Natl Acad Sci USA.109 3317.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Listings
Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.
JAN Code
529542-2MG:
Certificates of Analysis (COA)
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