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YIL781 HCl

Cat No.:V28374 Purity: ≥98%
YIL781 HCl is a potent, orally bioactive gastrophin receptor (GHSR) antagonist.
YIL781 HCl
YIL781 HCl Chemical Structure CAS No.: 1640226-17-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes

Other Forms of YIL781 HCl:

  • YIL781
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
YIL781 HCl is a potent, orally bioactive gastrophin receptor (GHSR) antagonist. YIL781 HCl improves glucose homeostasis in rats. YIL781 HCl inhibits ghrelin-induced calcium responses with pIC50s of 7.90 and 8.27, respectively.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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]. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85.

[2]. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530.

[3]. 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]. Ghrelin administered spinally increases the blood glucose level in mice. Peptides. 2014 Apr;54:162-5.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H29CLFN3O2
Molecular Weight
445.9574
Exact Mass
445.193
CAS #
1640226-17-0
Related CAS #
YIL781;875258-85-8
PubChem CID
74889155
Appearance
Off-white to light yellow solid powder
LogP
0
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
5
Heavy Atom Count
31
Complexity
632
Defined Atom Stereocenter Count
1
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
InChi Key
QQGRMONBDBMLSP-FERBBOLQSA-N
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
Chemical Name
6-(4-fluorophenoxy)-2-methyl-3-[[(3S)-1-propan-2-ylpiperidin-3-yl]methyl]quinazolin-4-one;hydrochloride
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~560.59 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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