YIL 781Ghrelin receptor (GHS-R1a) antagonist CAS# 875258-85-8 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 875258-85-8 | SDF | Download SDF |
| PubChem ID | 74889155 | Appearance | Powder |
| Formula | C24H29ClFN3O2 | M.Wt | 445.96 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in water | ||
| Chemical Name | 6-(4-fluorophenoxy)-2-methyl-3-[[(3S)-1-propan-2-ylpiperidin-3-yl]methyl]quinazolin-4-one;hydrochloride | ||
| SMILES | CC1=NC2=C(C=C(C=C2)OC3=CC=C(C=C3)F)C(=O)N1CC4CCCN(C4)C(C)C.Cl | ||
| Standard InChIKey | QQGRMONBDBMLSP-FERBBOLQSA-N | ||
| Standard InChI | InChI=1S/C24H28FN3O2.ClH/c1-16(2)27-12-4-5-18(14-27)15-28-17(3)26-23-11-10-21(13-22(23)24(28)29)30-20-8-6-19(25)7-9-20;/h6-11,13,16,18H,4-5,12,14-15H2,1-3H3;1H/t18-;/m0./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 | Ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo. |
YIL 781 Dilution Calculator
YIL 781 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2424 mL | 11.2118 mL | 22.4235 mL | 44.8471 mL | 56.0588 mL |
| 5 mM | 0.4485 mL | 2.2424 mL | 4.4847 mL | 8.9694 mL | 11.2118 mL |
| 10 mM | 0.2242 mL | 1.1212 mL | 2.2424 mL | 4.4847 mL | 5.6059 mL |
| 50 mM | 0.0448 mL | 0.2242 mL | 0.4485 mL | 0.8969 mL | 1.1212 mL |
| 100 mM | 0.0224 mL | 0.1121 mL | 0.2242 mL | 0.4485 mL | 0.5606 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Analysis of the ghrelin receptor-independent vascular actions of ulimorelin.[Pubmed:25687251]
Eur J Pharmacol. 2015 Apr 5;752:34-9.
Ulimorelin (TZP101) is a ghrelin receptor agonist that stimulates intestinal motility, but also reduces blood pressure in rodents and humans and dilates blood vessels. It has been proposed as a treatment for intestinal motility disorders. Here we investigated the mechanisms through which ulimorelin affects vascular diameter. Actions of ulimorelin on wall tension of rodent arteries were investigated and compared with other ghrelin receptor agonists. Saphenous, mesenteric and basilar arteries were obtained from Sprague-Dawley rats (male, 8 weeks) and saphenous arteries were obtained from wild type or ghrelin receptor null mice. These were mounted in myography chambers to record artery wall tension. Ulimorelin (0.03-30microM) inhibited phenylephrine-induced contractions of rat saphenous (IC50=0.6microM; Imax=66+/-5%; n=3-6) and mesenteric arteries (IC50=5microM, Imax=113+/-16%; n=3-4), but not those contracted by U46619, ET-1 or 60mM [K(+)]. Relaxation of phenylephrine-constricted arteries was not observed with ghrelin receptor agonists TZP102, capromorelin or AZP-531. In rat saphenous and basilar arteries, ulimorelin (10-100microM) and TZP102 (10-100microM) constricted arteries (EC50=9.9microM; Emax=50+/-7% and EC50=8microM; Emax=99+/-16% respectively), an effect not attenuated by the ghrelin receptor antagonist YIL 781 3microM or mimicked by capromorelin or AZP-531. In mesenteric arteries, ulimorelin, 1-10microM, caused a surmountable rightward shift in the response to phenylephrine (0.01-1000microM; pA2=5.7; n=3-4). Ulimorelin had similar actions in mouse saphenous artery from both wild type and ghrelin receptor null mice. We conclude that ulimorelin causes vasorelaxation through competitive antagonist action at alpha1-adrenoceptors and a constrictor action not mediated via the ghrelin receptor.
Minireview: Gut peptides: targets for antiobesity drug development?[Pubmed:19372201]
Endocrinology. 2009 Jun;150(6):2526-30.
Gut peptides play multiple roles in the controls of gastrointestinal function and in the initiation and termination of meals. Plasma levels of these peptides are differentially affected by the presence of nutrients in the digestive tract, and the patterns of peptide release are consistent with both their feeding stimulatory and inhibitory actions. A number of these peptide systems have been investigated as potential targets for antiobesity drug development. Progress has been made in developing long-acting peptide analogs and, in some cases, nonpeptide agonists and antagonists. Whether any individual approach will have significant long-term efficacy remains to be demonstrated. Approaches that target multiple systems may hold the most promise.
Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.[Pubmed:17656463]
Endocrinology. 2007 Nov;148(11):5175-85.
Ghrelin, through action on its receptor, GH secretagogue receptor type 1a (GHS-R1a), exerts a variety of metabolic functions including stimulation of appetite and weight gain and suppression of insulin secretion. In the present study, we examined the effects of novel small-molecule GHS-R1a antagonists on insulin secretion, glucose tolerance, and weight loss. Ghrelin dose-dependently suppressed insulin secretion from dispersed rat islets. This effect was fully blocked by a GHS-R1a antagonist. Consistent with this observation, a single oral dose of a GHS-R1a antagonist improved glucose homeostasis in an ip glucose tolerance test in rat. Improvement in glucose tolerance was attributed to increased insulin secretion. Daily oral administration of a GHS-R1a antagonist to diet-induced obese mice led to reduced food intake and weight loss (up to 15%) due to selective loss of fat mass. Pair-feeding experiments indicated that weight loss was largely a consequence of reduced food intake. The impact of a GHS-R1a antagonist on gastric emptying was also examined. Although the GHS-R1a antagonist modestly delayed gastric emptying at the highest dose tested (10 mg/kg), delayed gastric emptying does not appear to be a requirement for weight loss because lower doses produced weight loss without an effect on gastric emptying. Consistent with the hypothesis that ghrelin regulates feeding centrally, the anorexigenic effects of potent GHS-R1a antagonists in mice appeared to correspond with their brain exposure. These observations demonstrate that GHS-R1a antagonists have the potential to improve the diabetic condition by promoting glucose-dependent insulin secretion and promoting weight loss.
