GR 94800 (TFA)

GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].

Product Specifications

UNSPSC

12352209

Target

Neurokinin Receptor

Type

Peptides

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gr-94800-tfa.html

Solubility

10 mM in DMSO

Smiles

O=C(N1[C@H](CCC1)C(N2[C@@H](CCC2)C(N[C@H](C(N)=O)CCCC)=O)=O)[C@H](CC3=CC=CC=C3)NC([C@H](NC([C@H](C)NC([C@H](C)NC(C4=CC=CC=C4)=O)=O)=O)CC5=CNC6=CC=CC=C56)=O.OC(C(F)(F)F)=O.[x]

Molecular Formula

C49H61N9O8·xC2HF3O2

Molecular Weight

904.06 (free base)

References & Citations

[1]A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35 (14) :2582-91.|[2]M A Matuszek, et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur J Pharmacol. 1998 Jul 3;352 (1) :103-9.|[3]Stephen D Tichenor, et al. Excitatory motor innervation in the canine rectoanal region: role of changing receptor populations. Br J Pharmacol. 2002 Dec;137 (8) :1321-9.