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YIL 781

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Catalog No. T23543Cas No. 875258-85-8

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.

YIL 781

YIL 781

🥰Excellent
Purity: 99.3%
Catalog No. T23543Cas No. 875258-85-8
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 SizePriceAvailabilityQuantity
1 mg$44In Stock
5 mg$97In Stock
10 mg$155In Stock
25 mg$328In Stock
50 mg$493In Stock
100 mg$689In Stock
1 mL x 10 mM (in DMSO)$125In Stock
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Purity:99.3%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight409.5
FormulaC24H28FN3O2
Cas No.875258-85-8
SmilesO=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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.4420 mL12.2100 mL24.4200 mL122.1001 mL
5 mM0.4884 mL2.4420 mL4.8840 mL24.4200 mL
10 mM0.2442 mL1.2210 mL2.4420 mL12.2100 mL
20 mM0.1221 mL0.6105 mL1.2210 mL6.1050 mL
50 mM0.0488 mL0.2442 mL0.4884 mL2.4420 mL

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