Kisspeptin 234
Kisspeptin 234 is a kisspeptin receptor antagonist, with the ability to antagonize kisspeptin-10-induced activation of gpr-54. Kisspeptin binds to its cognate receptor (i.e. gpr-54) on neurons that produce gonadotropin-releasing hormone (GnRH), and stimulates their activity, which in turn sends an obligatory signal for GnRH secretion, thereby gating down-stream events supporting reproduction. The development of kisspeptin receptor antagonists may provide a valuable tool for exploring the physiological and pathophysiological roles of kisspeptin in the regulation of reproduction, and could serve as a potential therapeutic agent for treating hormone-dependent disorders of reproduction, such as precocious puberty, endometriosis, as well as metastatic prostate cancer.
Reference:
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.
| Physical Appearance | White lyophilised solid |
| Storage | Store at -20°C |
| M.Wt | 1295.42 |
| Cas No. | 1145998-81-7 |
| Formula | C63H78N18O13 |
| Solubility | insoluble 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 |
| SDF | Download SDF |
| Canonical SMILES | C[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 Condition | Small 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. |
| Cell experiment:[1] | |
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Cell lines |
GnRH neurons |
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Reaction Conditions |
100 pM ~ 10 μM kisspeptin 234 |
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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] | |
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Animal models |
Pubertal female rhesus monkeys |
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Dosage form |
10 nM Infusion of 10 nM kisspeptin 234 over 30 min through a microdialysis probe located in the stalk-median eminence region |
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Applications |
Kisspeptin 234 was shown to reduce pulsatile GnRH secretion in female pubertal monkeys, which supports a key role of kisspeptin in puberty onset. |
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Note |
The technical data provided above is for reference only. |
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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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Quality Control & MSDS
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Chemical structure
