YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
| Molecular Weight | 409.5 |
| Formula | C24H28FN3O2 |
| CAS Number | 875258-85-8 |
| Form | Solid |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Ghrelin Receptor/GHSR Products |
|---|
| des-Gln14-Ghrelin
des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. |
| Obestatin(rat)
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. |
| Human growth hormone-releasing factor
Human growth hormone-releasing factor (Growth Hormone Releasing Factor human) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary. |
| [His1, Nle27] GHRF (1-32), amide, human
[His1,Nle27] GHRF (1-32), amide, human is a Growth hormone releasing hormone (GHRH) analog. |
| Obestatin(rat) TFA
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. |
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