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KISS1R antagonist P234

Chemical Structure : KISS1R antagonist P234

CAS No.:

KISS1R antagonist P234 (GPR54 antagonist P234, Peptide 234)

Catalog No.: PC-21174Not For Human Use, Lab Use Only.

KISS1R antagonist P234 (GPR54 antagonist P234, Peptide P234) is a potent GPR54 receptor antagonist with binding IC50 of 2.7 nM in competition with 125I-kisspeptin-10, blocks the stimulatory effects of kisspeptin on hypothalamus-pituitary-gonadal (HPG) axis.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KISS1R antagonist P234 (GPR54 antagonist P234, Peptide P234) is a potent GPR54 receptor antagonist with binding IC50 of 2.7 nM in competition with 125I-kisspeptin-10, blocks the stimulatory effects of kisspeptin on hypothalamus-pituitary-gonadal (HPG) axis.
Peptide P234 potently inhibits 10 nM kisspeptin-10 stimulation of IP by 93%, with an IC50 of 7 nM and has no intrinsic IP stimulation.
Peptide 234 (1 nM) antagonizes kisspeptin-10 excitation of GnRH neurons.
Peptide 234 inhibits pulsatile GnRH release in pubertal female rhesus monkeys.
Peptide 234 inhibits kisspeptin-10 stimulated LH in intact male rats and the increase in LH after castration.

Physicochemical Properties

M.Wt
Formula
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

Ac[(D)-A]NWNGFG[(D)-W]RF

References

1. Fariba Mahmoudi, et al. Int J Endocrinol Metab. 2014 Jan 5;12(1):e12554.

2. Antonia K Roseweir, et al. J Neurosci. 2009 Mar 25;29(12):3920-9.

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