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
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M.Wt
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Formula
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Ac[(D)-A]NWNGFG[(D)-W]RF
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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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