| Name | YIL 781 |
| Description | YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 μM). YIL 781 improves glucose homeostasis in vivo and in vitro by blocking ghrelin secretion. |
| In vitro | Post-transcriptional suppression by Ghsr siRNA transfection and treatment with GHS-R antagonist, YIL781, both significantly attenuated the effects of ghrelin in RGC-5 cells.[1] |
| In vivo | YIL781 (ghrelin receptor antagonist; from 0.1 to 5 μg; i.t. pretreatment) markedly attenuated the ghrelin-induced hyperglycemic effect. The plasma insulin level was increased by ghrelin. The enhanced plasma insulin level by ghrelin was reduced by i.t. pretreatment with YIL781.[2] With YIL781 pretreatment, the accumulated radioactivity in the pancreas 15-60min after [11C]3 injection was significantly decreased to 78% of control.[3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.88 mM), Sonication is recommended. DMSO : 150 mg/mL (366.3 mM), Sonication is recommended. H2O : 40.1 mg/mL (97.92 mM), Sonication is recommended.
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| Keywords | YIL-781 | YIL781 | YIL 781 | GHS-R1a |
| Inhibitors Related | Ibutamoren Mesylate | AnaMorelin hydrochloride | Capromorelin Tartrate | Anamorelin | Ibutamoren | CJC-1295 acetate(863288-34-0 free base) | L-692429 | Obestatin (human) | JMV 2959 hydrochloride (925238-89-7 free base) | Obestatin (rat) acetate | TM-N1324 | Cortistatin-8 acetate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library | Anti-Cancer Compound Library |