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Kisspeptin 234

Catalog No.
B5489
A kisspeptin receptor antagonist
Grouped product items
SizePriceStock Qty
1mg
$438.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

Kisspeptin 234 (CAS 1145998-81-7) is a selective antagonist targeting the kisspeptin receptor GPR-54. The molecule inhibits activation of GPR-54 induced by kisspeptin-10, thereby attenuating downstream signaling events critical for gonadotropin-releasing hormone (GnRH) secretion. By modulating kisspeptin-GPR-54 interactions, Kisspeptin 234 provides researchers a valuable pharmacological tool to investigate physiological mechanisms underlying reproductive hormone control and pathologies including precocious puberty, endometriosis, and metastatic prostate cancer.

Product Citation

Chemical Properties

Physical AppearanceWhite lyophilised solid
StorageStore at -20°C
M.Wt1295.42
Cas No.1145998-81-7
FormulaC63H78N18O13
Solubilityinsoluble in DMSO; insoluble in EtOH; ≥4.44 mg/mL in H2O with ultrasonic
Chemical Name(S,Z)-N'1-((6S,7Z,9R,10Z,13Z,15S,16Z,19Z,21S,22Z,24S)-9-((1H-indol-3-yl)methyl)-1-amino-15-benzyl-8,11,14,17,20,23-hexahydroxy-6-((Z)-hydroxy(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)methyl)-21-(2-hydroxy-2-iminoethyl)-1-imino-25-(1H-indol-3-yl)-2
SDFDownload SDF
Canonical SMILESC[C@](/N=C(O)/C)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC1=CC=CC=C1)([H])CCCNC(N)=N)([H])CC2=CNC3=CC=CC=C23)([H])CC4=CC=CC=C4)([H])CC(O)=N)([H])CC5=CNC6=CC=CC=C56
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]

Cell lines

GnRH neurons

Reaction Conditions

100 pM ~ 10 μM kisspeptin 234

Applications

Kisspeptin 234 substantially inhibited kisspeptin-10 stimulation of inositol phosphate, with an IC50 value of 7 nM. At the doses of 1, 10 and 100 nM, kisspeptin 234 significantly reduced kisspeptin-10-induced GnRH neuron firing activity.

Animal experiment:[1]

Animal models

Pubertal female rhesus monkeys

Dosage form

10 nM

Infusion of 10 nM kisspeptin 234 over 30 min through a microdialysis probe located in the stalk-median eminence region

Applications

Kisspeptin 234 was shown to reduce pulsatile GnRH secretion in female pubertal monkeys, which supports a key role of kisspeptin in puberty onset.

Note

The technical data provided above is for reference only.

References:

1. Roseweir AK, Kauffman AS, Smith JT, et al. Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation. Journal of Neuroscience, 2009, 29(12): 3920-3929.

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