| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
YIL781 specifically targets GHS-R1a, the ghrelin receptor, a G protein-coupled receptor that mediates the effects of ghrelin on growth hormone release, appetite, and glucose metabolism. By acting as a potent and selective antagonist, YIL781 blocks ghrelin signaling. This makes it a valuable tool for investigating the physiological and pathophysiological roles of ghrelin.
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| ln Vitro |
Ghrelin CRC exhibits a concentration-dependent parallel right shift when exposed to YIL781 (10–300 nM); at 100 and 300 nM, there is a little but statistically significant suppression of the maximal response, which reaches roughly 90% of the agonist-like peak response [3].
In vitro, YIL781 is a potent and selective antagonist of GHS-R1a. Its high affinity (Ki = 17 nM) and selectivity over the motilin receptor (Ki = 6 μM) confirm its specificity. In cellular assays, it effectively blocks ghrelin-induced signaling. For example, it significantly attenuates the effects of ghrelin in RGC-5 cells. |
| ln Vivo |
YIL781 (0.1-5 μg/5 μL) reduces the increase in blood glucose levels brought on by ghrelin. Blood glucose levels are not impacted by YIL781 alone [4].
In vivo, YIL781 is an orally bioactive compound that improves glucose homeostasis. It blocks ghrelin secretion and reduces insulin secretion. In a mouse model, YIL781 (0.1 to 5 μg; intracerebroventricular pretreatment) significantly attenuated the hyperglycemic effect caused by ghrelin and reduced the ghrelin-enhanced increase in plasma insulin levels. |
| Enzyme Assay |
For non-cellular in vitro receptor binding assays, YIL781 is characterized using radioligand binding techniques with membrane preparations from cells expressing the ghrelin receptor (GHS-R1a) and the motilin receptor. These assays determine its binding affinity (Ki = 17 nM for GHS-R1a) and confirm its selectivity. Such studies are critical for establishing the compound's high potency and specificity.
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| Cell Assay |
For in vitro cellular assays, the activity of YIL781 is evaluated in cells expressing the ghrelin receptor. A typical assay measures its ability to inhibit ghrelin-induced signaling, such as the mobilization of intracellular calcium. By blocking the receptor, YIL781 prevents the increase in calcium typically seen upon ghrelin stimulation.
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| Animal Protocol |
In vivo animal studies with YIL781 are conducted to study its effects on glucose homeostasis and ghrelin signaling. In mice, it is administered via intracerebroventricular (ICV) injection to study its effects on the central ghrelin system. Its effects on glucose and insulin levels are measured to assess its impact on metabolism and validate its mechanism of action.
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| ADME/Pharmacokinetics |
YIL781 is orally bioactive, indicating favorable oral bioavailability. It is soluble in DMSO and water at 40.1 mg/mL, which aids in formulation for both in vitro and in vivo applications. Its pharmacokinetic properties, such as half-life and clearance, are not detailed in the search results, but its oral activity suggests it is suitable for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for YIL781 are not extensively detailed. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References |
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| Additional Infomation |
An appetite suppressant and weight loss promoter; structure as described in the first source.
YIL781 is a potent and selective ghrelin receptor (GHS-R1a) antagonist with a Ki of 17 nM. It shows weak affinity for the motilin receptor (Ki = 6 μM). It is orally bioactive and improves glucose homeostasis by blocking ghrelin secretion. YIL781 is a key research tool for studying the ghrelin system, metabolism, and diabetes. |
| Molecular Formula |
C24H28FN3O2
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|---|---|
| Molecular Weight |
409.50
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| Exact Mass |
445.193
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| CAS # |
875258-85-8
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| Related CAS # |
YIL781 hydrochloride;1640226-17-0
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| PubChem CID |
23631116
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.496
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
632
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=NC2=C(C=C(C=C2)OC3=CC=C(C=C3)F)C(=O)N1C[C@H]4CCCN(C4)C(C)C
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| InChi Key |
FRKXOBMDEXCHHD-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C24H28FN3O2/c1-16(2)27-12-4-5-18(14-27)15-28-17(3)26-23-11-10-21(13-22(23)24(28)29)30-20-8-6-19(25)7-9-20/h6-11,13,16,18H,4-5,12,14-15H2,1-3H3/t18-/m0/s1
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| Chemical Name |
6-(4-fluorophenoxy)-2-methyl-3-[[(3S)-1-propan-2-ylpiperidin-3-yl]methyl]quinazolin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (244.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4420 mL | 12.2100 mL | 24.4200 mL | |
| 5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | |
| 10 mM | 0.2442 mL | 1.2210 mL | 2.4420 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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