H-ARG-ARG-ARG-ARG-ARG-ARG-ARG-ARG-ARG-OH

Product NameH-ARG-ARG-ARG-ARG-ARG-ARG-ARG-ARG-ARG-OH
CAS143413-47-2
MFC54H110N36O10
MW1423.69
EINECS
MOL File143413-47-2.mol

Chemical Properties

Density	1.60±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
Sequence	H-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-OH

Usage And Synthesis

Uses

(Arg)9 (Nona-L-arginine) is a cell-penetrating peptide (CPP) made up of 9 arginine residues, which is an inhibitor of serine endoprotease Furin. (Arg)9 has neuroprotective property, exhibits neuroprotective activity with an IC50 of 0.78 μM in the glutamic acid model[1][2].

Biological Activity

(Arg)9 (Nona-L-arginine; Peptide R9) is a cell-permeable polypeptide with IC50 value of 0.78 μM for neuroprotection in a glutamate model experimental model.

in vitro

Poly-arginine (eg (Arg)9) and arginine-rich peptides (eg TAT, penetratin), which belong to a class of peptides with cell-penetrating properties are neuroprotective. It provides significant neuroprotection in a dose–response manner following glutamic acid exposure (IC ₅₀ =0.78 μM). Following kainic acid exposure, (Arg)9 is neuroprotective, but less effective than in the glutamic acid model (IC ₅₀ =0.81 μM). (Arg)9 also shows neuroprotection following in vitro ischemia (IC ₅₀ =6 μM).

in vivo

(Arg)9) (D-isoform) is neuroprotective in rat stroke models. (Arg)9) is highly neuroprotective, with efficacy increasing with increasing arginine content, has the capacity to reduce glutamic acid-induced neuronal calcium influx and requires heparan sulfate preotoglycan-mediated endocytosis to induce a neuroprotective effect. (Arg)9) (D-isoform) administered intravenously at a dose of 1000 nmol/kg 30 min after reduces permanent middle cerebral artery occlusion (MCAO) infarct volume .

target

IC50: 0.78 μM (neuroprotection)

References

[1] Cameron A, et al. Polyarginines are potent furin inhibitors. J Biol Chem. 2000 Nov 24;275(47):36741-9. DOI:10.1074/jbc.M003848200
[2] Meloni BP, et, al. The neuroprotective efficacy of cell-penetrating peptides TAT, penetratin, Arg-9, and Pep-1 in glutamic acid, kainic acid, and in vitro ischemia injury models using primary cortical neuronal cultures. Cell Mol Neurobiol. 2014 Mar;34(2):173-81. DOI:10.1007/s10571-013-9999-3
[3] Meloni BP, et, al. Poly-arginine and arginine-rich peptides are neuroprotective in stroke models. J Cereb Blood Flow Metab. 2015 Jun;35(6):993-1004. DOI:10.1038/jcbfm.2015.11

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