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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $44 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $328 | In Stock | |
50 mg | $493 | In Stock | |
100 mg | $689 | In Stock | |
1 mL x 10 mM (in DMSO) | $125 | In Stock |
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] |
Molecular Weight | 409.5 |
Formula | C24H28FN3O2 |
Cas No. | 875258-85-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40.1 mg/mL (90.0 mM) H2O: 40.1 mg/mL (90.0 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO/H2O
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