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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 | USA Warehouse | Global Warehouse | 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 |
| Smiles | O=C1C=2C(N=C(C)N1C[C@@H]3CN(C(C)C)CCC3)=CC=C(OC4=CC=C(F)C=C4)C2 |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40.1 mg/mL (97.92 mM), Sonication is recommended. H2O: 40.1 mg/mL (97.92 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.88 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO/H2O
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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