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100mg | ||
250mg | ||
500mg |
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].
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ln Vivo |
YIL781 (0.1-5 μg/5 μL) inhibits ghrelin-induced elevation of blood glucose levels. YIL781 alone does not impact blood glucose levels [4].
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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). |
References |
[1]. William P Esler, et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85.
[2]. Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530. [3]. Elisabetta Perdonà, et al. Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors. Eur J Pharmacol. 2011 Jan 10;650(1):178-83. [4]. Yun-Beom Sim, et al. Ghrelin administered spinally increases the blood glucose level in mice. Peptides. 2014 Apr;54:162-5. |
Molecular Formula |
C24H29CLFN3O2
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Molecular Weight |
445.9634
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Exact Mass |
409.2166
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CAS # |
1640226-17-0
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Related CAS # |
YIL781;875258-85-8
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SMILES |
Cl[H].FC1C([H])=C([H])C(=C([H])C=1[H])OC1C([H])=C([H])C2=C(C=1[H])C(N(C(C([H])([H])[H])=N2)C([H])([H])[C@@]1([H])C([H])([H])C([H])([H])C([H])([H])N(C([H])(C([H])([H])[H])C([H])([H])[H])C1([H])[H])=O
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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.