| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
YIL781 targets the growth hormone secretagogue receptor 1a (GHS-R1a), the receptor for the orexigenic hormone ghrelin. As an antagonist, it blocks ghrelin-mediated signaling. It is selective for GHS-R1a over the motilin receptor (Ki = 6 µM) and a panel of 30 receptors and enzymes (Kis >10 µM). YIL781 inhibits ghrelin-induced calcium responses.
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| ln Vitro |
YIL781 (10-300 nM) causes ghrelin CRC to exhibit a concentration-dependent parallel right shift. At 100 and 300 nM, there is a modest but statistically significant suppression of the peak response, which reaches roughly 90% of the agonist-like maximal response [3].
In vitro, YIL781 is a potent GHS-R1a antagonist with a Ki of 0.017 µM for GHS-R1a. It inhibits ghrelin-induced calcium responses with pIC₅₀ values of 7.90 and 8.27. The compound shows high selectivity for GHS-R1a over the motilin receptor (Ki = 6 µM) and over a panel of 30 receptors and enzymes (Kis >10 µM). |
| ln Vivo |
YIL781 (0.1-5 μg/5 μL) inhibits the increase in blood glucose levels brought on by ghrelin. Blood glucose levels are not impacted by YIL781 alone [4].
In vivo, YIL781 hydrochloride improves glucose homeostasis in rats. As an orally bioactive ghrelin receptor antagonist, it reduces food intake and modulates metabolic processes. Its ability to improve glucose homeostasis suggests potential applications in studying metabolic syndrome, diabetes, and appetite regulation. |
| Enzyme Assay |
In vitro receptor binding assays for YIL781 are performed using membrane preparations expressing human GHS-R1a. Radioligand competition binding assays are used to measure the compound's affinity for GHS-R1a, and the Ki (0.017 µM) is calculated from competition curves. Selectivity is assessed by testing the compound against a panel of other receptors and enzymes.
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| Cell Assay |
In vitro cellular assays for YIL781 are performed using cells expressing GHS-R1a. Cells are treated with ghrelin in the presence of increasing concentrations of the compound. Calcium mobilization is measured using fluorescence-based calcium indicators. The pIC₅₀ values (7.90 and 8.27) for inhibition of ghrelin-induced calcium responses are calculated from concentration-response curves.
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| Animal Protocol |
Animal/Disease Models: Conscious mice [4].
Doses: 0.1 to 5 micrograms/5 microliters. Route of Administration: Intrathecal (it) injection. Experimental Results: Ghrelin-induced upregulation of blood glucose levels was attenuated (F = 0.7506; P = 0.5729) (YIL781 5 g + ghrelin 5 g -9.1%, 30 min; -14.9%, 60 min). YIL781 treatment alone did not affect blood glucose levels (F = 0.8160; P = 0.5095). In vivo animal experiments for YIL781 are conducted in rat models. A typical protocol involves oral administration of the compound to rats, followed by assessment of glucose tolerance, insulin sensitivity, and food intake. Glucose homeostasis is evaluated by measuring blood glucose levels during glucose tolerance tests. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of YIL781 hydrochloride have been characterized in part. The compound has a molecular weight of 445.96 and molecular formula C₂₄H₂₉ClFN₃O₂. It is supplied with purity ≥98%. It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. It is shipped with blue ice.
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| Toxicity/Toxicokinetics |
Toxicological data for YIL781 hydrochloride are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
YIL781 hydrochloride is a potent GHS-R1a antagonist with a Ki of 0.017 µM. It is selective for GHS-R1a over the motilin receptor and a panel of other receptors and enzymes. It improves glucose homeostasis in rats and is used in endocrinology and neurobiology research to study ghrelin receptor function, appetite control, and energy metabolism. This product is for research use only.
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| Molecular Formula |
C24H29CLFN3O2
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|---|---|
| Molecular Weight |
445.9574
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| Exact Mass |
445.193
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| CAS # |
1640226-17-0
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| Related CAS # |
YIL781;875258-85-8
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| PubChem CID |
74889155
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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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.Cl
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| InChi Key |
QQGRMONBDBMLSP-FERBBOLQSA-N
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| InChi Code |
InChI=1S/C24H28FN3O2.ClH/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;1H/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;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~250 mg/mL (~560.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.66 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 20.8 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: ≥ 2.08 mg/mL (4.66 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 20.8 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: ≥ 2.08 mg/mL (4.66 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 | 2.2424 mL | 11.2118 mL | 22.4235 mL | |
| 5 mM | 0.4485 mL | 2.2424 mL | 4.4847 mL | |
| 10 mM | 0.2242 mL | 1.1212 mL | 2.2424 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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