Kisspeptin 234Kisspeptin receptor antagonist; kisspeptin 10 analog CAS# 1145998-81-7 |
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Quality Control & MSDS
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| Cas No. | 1145998-81-7 | SDF | Download SDF |
| PubChem ID | 90488890 | Appearance | Powder |
| Formula | C63H78N18O13 | M.Wt | 1295.42 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 1 mg/ml in 20% acetonitrile / water | ||
| Sequence | Ac-ANWNGFGWRF-NH2 (Modifications: Ala-1 = D-Ala & N-terminal Ac, Trp-8 = D-Trp, Phe-10 = C-terminal amide) | ||
| SMILES | CC(C(=O)NC(CC(=O)N)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(=O)N)C(=O)NCC(=O)NC(CC3=CC=CC=C3)C(=O)NCC(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)N)NC(=O)C | ||
| Standard InChIKey | IUPKBWSKNCAQJQ-JYYYXURSSA-N | ||
| Standard InChI | InChI=1S/C63H78N18O13/c1-34(74-35(2)82)56(88)79-50(29-52(65)84)62(94)80-48(27-39-31-71-43-21-12-10-19-41(39)43)61(93)81-49(28-51(64)83)58(90)73-32-53(85)75-46(25-37-16-7-4-8-17-37)57(89)72-33-54(86)76-47(26-38-30-70-42-20-11-9-18-40(38)42)60(92)77-44(22-13-23-69-63(67)68)59(91)78-45(55(66)87)24-36-14-5-3-6-15-36/h3-12,14-21,30-31,34,44-50,70-71H,13,22-29,32-33H2,1-2H3,(H2,64,83)(H2,65,84)(H2,66,87)(H,72,89)(H,73,90)(H,74,82)(H,75,85)(H,76,86)(H,77,92)(H,78,91)(H,79,88)(H,80,94)(H,81,93)(H4,67,68,69)/t34-,44+,45+,46+,47-,48+,49+,50+/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | kisspeptin receptor (KISS1, GPR54) antagonist; kisspeptin-10 analog. Inhibits kisspeptin-10 stimulation of inositol phosphate (IP) (IC50 = 7 nM) and release of gonadotrophin-releasing hormone (GnRH). |
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Presence and function of kisspeptin/KISS1R system in swine ovarian follicles.[Pubmed:29698886]
Theriogenology. 2018 Jul 15;115:1-8.
Kisspeptin and its receptor KISS1R are involved in the neuroendocrine regulation of mammalian reproduction and their role on follicular development and function can be hypothesized. The present work was designed to confirm the immunopresence of kisspeptin and its receptor in the ovary of swine and to study the effects of kisspeptin 10 and its antagonist, Kisspeptin 234, on main functional parameters of granulosa cells (i.e. cell proliferation, steroid production, and redox status) as well as their modulatory action on angiogenesis. The immunopresence of kisspeptin and KISS1R were detected in granulosa cells. Kisspeptin 10 stimulated progesterone in vitro production, thus indirectly suggesting that it can have a role in the luteinization process of granulosa cells. Kisspeptin 10 displayed potentiating effects on non-enzymatic scavenging activity, thus supporting its involvement in the control of the antioxidant defense system of ovarian follicles. In addition, results from the angiogenesis bioassay suggest that kisspeptin may have a role in the physiological development of new ovarian vessels. Additional studies are needed to confirm the functional significance of the kisspeptin/KISS1R system within the swine ovary.
Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation.[Pubmed:19321788]
J Neurosci. 2009 Mar 25;29(12):3920-9.
Neurons that produce gonadotropin-releasing hormone (GnRH) are the final common pathway by which the brain regulates reproduction. GnRH neurons are regulated by an afferent network of kisspeptin-producing neurons. Kisspeptin binds to its cognate receptor on GnRH neurons and stimulates their activity, which in turn provides an obligatory signal for GnRH secretion, thus gating down-stream events supporting reproduction. We have developed kisspeptin antagonists to facilitate the direct determination of the role of kisspeptin neurons in the neuroendocrine regulation of reproduction. In vitro and in vivo studies of analogues of kisspeptin-10 with amino substitutions have identified several potent and specific antagonists. A selected antagonist was shown to inhibit the firing of GnRH neurons in the brain of the mouse and to reduce pulsatile GnRH secretion in female pubertal monkeys; the later supporting a key role of kisspeptin in puberty onset. This analog also inhibited the kisspeptin-induced release of luteinizing hormone (LH) in rats and mice and blocked the postcastration rise in LH in sheep, rats, and mice, suggesting that kisspeptin neurons mediate the negative feedback effect of sex steroids on gonadotropin secretion in mammals. The development of kisspeptin antagonists provides a valuable tool for investigating the physiological and pathophysiological roles of kisspeptin in the regulation of reproduction and could offer a unique therapeutic agent for treating hormone-dependent disorders of reproduction, including precocious puberty, endometriosis, and metastatic prostate cancer.
