TT-OAD2

Names

[ Name ]:
TT-OAD2

Biological Activity

[Description]:

TT-OAD2 is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC50 of 5 nM. TT-OAD2 has the potential for diabetes treatment[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> Glucagon Receptor

[Target]

EC50: 5 nM (GLP-1 receptor)[2]

[In Vitro]

TT-OAD2 (0-10 μM) inhibits GLP-1- and oxyntomodulin-mediated cAMP, calcium, pERK1/2 and β-arrestin responses in a concentration-dependent manner in HEK293A cells[1].

[In Vivo]

TT-OAD2 (3 mg/kg; intravenous injection; male human GLP-1 receptor knock-in and knockout mice) treatment induces plasma insulin in an acute IVGTT on humanized GLP-1R knock-in (KI) and GLP-1R knockout (KO) mice[1]. Animal Model: Male human GLP-1 receptor knock-in and knockout mice (6-11 months of age) with intravenous glucose tolerance tests[1] Dosage: 3 mg/kg Administration: Intravenous injection (Single dose) Result: Induced plasma insulin.

[References]

[1]. Zhao P, et al. Activation of the GLP-1 receptor by a non-peptidic agonist. Nature. 2020 Jan;577(7790):432-436.

[2]. Transtech Pharma, et al. Substituted azoanthracene derivatives, pharmaceutical compositions, and methods of use thereof. WO2010114824A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₀H₄₉Cl₄N₃O₆

[ Molecular Weight ]:
929.75

Related Compounds

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