| Identification | Back Directory | [Name]
YIL 781 hydrochloride | [CAS]
1640226-17-0 | [Synonyms]
YIL781 HCl
YIL781 hydrochloride,YIL-781 hydrochloride | [Molecular Formula]
C24H29ClFN3O2 | [MDL Number]
MFCD19690924 | [MOL File]
1640226-17-0.mol | [Molecular Weight]
445.96 |
| Hazard Information | Back Directory | [Uses]
YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively[1][2][3][4]. | [in vivo]
YIL781 (0.1 to 5 μg/5 μl) attenuates ghrelin-induced up-regulation of the blood glucose level. The
i.t. treatment with YIL781 alone does not affect the blood glucose level (F = 0.8160; P = 0.5095)[4]. | Animal Model: | Conscious mice[4]. | | Dosage: | 0.1 to 5 μg/5 μl. | | Administration: | Intrathecal (i.t.) injection. | | Result: | Attenuated ghrelin-induced up-regulation of the blood glucose level (F = 0.7506; P = 0.5729) (YIL781 5 g + ghrelin 5 g ?9.1% at 30 min; ?14.9% at 60 min).
The i.t. treatment with YIL781 alone did not affect the blood glucose level (F = 0.8160; P = 0.5095).
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| [storage]
Store at -20°C | [References]
[1] William P Esler, et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85. DOI:10.1210/en.2007-0239
[2] Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530. DOI:10.1210/en.2009-0003
[3] Elisabetta Perdonà, et al. Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors. Eur J Pharmacol. 2011 Jan 10;650(1):178-83. DOI:10.1016/j.ejphar.2010.10.042
[4] Yun-Beom Sim, et al. Ghrelin administered spinally increases the blood glucose level in mice. Peptides. 2014 Apr;54:162-5. DOI:10.1016/j.peptides.2014.01.015 |
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| Company Name: |
R&D Systems, Inc
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| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
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