FE 205030 | CGRP antagonist | Probechem Biochemicals

Chemical Structure : FE 205030

FE 205030 (FE205030)

Catalog No.: PC-72787Not For Human Use, Lab Use Only.

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.

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Biological Activity

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.
FE 205030 displays>100,000 fold against hAM1R and >6363 fold against hAM2R tested in Human CGRP, AM1R and AM2R receptor cAMP assays.
FE 205030 inhibited CGRP-induced vasodilation in isolated human mesenteric resistance arteries in an ex vivo isometric myograph study; effectively blocked CGRP-induced vasodilation with a pA2 of 9.3.
FE 205030 is a first in class injectable fast acting selective and potent agent for the treatment of acute episodic migraine.

Physicochemical Properties

M.Wt	1397.59
Formula	C64H84N16O16S2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Oxazole-2-carbonyl-D-Val-Phe(2-Cbm)-c(Cys-Orn(iPr)-Asp-Val-Gly-Pro-Phe-Cys)-3Pal- NH2

References

1. Karthik Srinivasan, et al. J Pharm Sci. 2022 Jan;111(1):247-261.

FE 205030 (FE205030)

Biological Activity

Physicochemical Properties

References

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