An antagonist of GHS-R1a
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Alternative(s)
45211YIL 781
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YIL 781 (hydrochloride)

Item No. 29217

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(4-fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone, monohydrochloride
CAS Number
1640226-17-0
Molecular Formula
C24H28FN3O2 • HCl
Formula Weight
446.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 100 mM
SMILES
FC1=CC=C(OC2=CC=C(N=C(C)N(C[C@H]3CCCN(C(C)C)C3)C4=O)C4=C2)C=C1.Cl
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
InChi Key
QQGRMONBDBMLSP-FERBBOLQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

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    10 mg

    $217

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    25 mg

    $488

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    YIL 781 is an antagonist of the growth hormone secretagogue receptor 1a (GHS-R1a; Ki = 0.017 µM).1 It is selective for GHS-R1a over the motilin receptor (Ki = 6 µM) and a panel of 30 receptors and enzymes (Kis = >10 µM). YIL 781 (1 µM) prevents ghrelin-induced decreases in insulin secretion in glucose-stimulated isolated rat pancreatic islets. It increases plasma insulin levels and decreases blood glucose levels in an intraperitoneal glucose tolerance test in rats when administered at doses of 0.3 or 10 mg/kg, respectively. YIL 781 (10 and 20 mg/kg) inhibits cocaine-induced hyperlocomotion in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Esler, W.P., Rudolph, J., Claus, T.H., et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148(11), 5175-5185 (2007).

    2. Toth, K., Slosky, L.M., Pack, T.F., et al. Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2. Synapse 72(1), e22012 (2018).