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Adomeglivant

CAS No. : 1488363-78-5

MCE 站：Adomeglivant

产品活性：Adomeglivant (LY2409021) 是一种有效的选择性胰高血糖素受体 (GluR) 变构拮抗剂。Adomeglivant 广泛应用于 2 型糖尿病的研究。

研究领域：GPCR/G Protein

作用靶点：Glucagon Receptor

In Vitro: Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells.
Adomeglivant fails to block cAMP-elevating actions of adenosine.
Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R.

In Vivo: Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avp^ires-Cre+ mice. (CNO is a specific, pharmacologically inert agonist for hM3Dq-induced membrane depolarisation and increased the firing rate in hM3Dq-expressing arginine-vasopressin (AVP) neurons.)

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