YIL781 free base · Synonyms: YIL-781 · YIL 781

YIL781 is a potent and orally active ghrelin receptor antagonist.

For research use only. Not for human or veterinary use.

Target GHSR

Research area Metabolic Disease

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Data Sheet SDS COA

YIL781 structure

CAS No.: 875258-85-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 560.00	BP-02149-100mg	In stock	Get quote
250 mg	USD 1,100.00	BP-02149-250mg	In stock	Get quote
500 mg	USD 1,750.00	BP-02149-500mg	In stock	Get quote
1 g	USD 2,800.00	BP-02149-1g	In stock	Get quote
2 g	USD 4,200.00	BP-02149-2g	In stock	Get quote

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Description

YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively .

Biological activity

In Vitro YIL781 (10-300 nM) induces a concentration-dependent parallel rightward shift of the ghrelin CRC with a slight but statistically significant depression of the maximal response at 100 and 300 nM, reaching a similar agonist maximal response of approximately 90%. In Vivo YIL781 (0.1 to 5 μg/5 μl) attenuates ghrelin-induced up-regulation of the blood glucose level. The i.t. treatment with YIL781 alone does not affect the blood glucose level (F = 0.8160; P = 0.5095).

Identifiers

SMILES: CC1=NC2=C(C=C(C=C2)OC3=CC=C(C=C3)F)C(=O)N1C[C@H]4CCCN(C4)C(C)C
InChIKey: FRKXOBMDEXCHHD-SFHVURJKSA-N

Specifications

MW (average): 409.4964
Formula: C₂₄H₂₈FN₃O₂
CAS No.: 875258-85-8
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

Same research area

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