LGD-6972

Names

[ CAS No. ]:
1207989-09-0

[ Name ]:
LGD-6972

[Synonym ]:
Ethanesulfonic acid, 2-[[4-[(2R)-2-[4'-(1,1-dimethylethyl)[1,1'-biphenyl]-4-yl]-3-oxo-3-[(2',4',6'-trimethyl[1,1'-biphenyl]-4-yl)amino]propyl]benzoyl]amino]-
2-[(4-{(2R)-2-[4'-(2-Methyl-2-propanyl)-4-biphenylyl]-3-oxo-3-[(2',4',6'-trimethyl-4-biphenylyl)amino]propyl}benzoyl)amino]ethanesulfonic acid
6IJ842I0Z2

Biological Activity

[Description]:

LGD-6972 is a glucagon receptor antagonist.

[Related Catalog]:

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

Research Areas >> Metabolic Disease

[In Vivo]

LGD-6972 has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. Dose-dependent decreases in fasting plasma glucose are observed in all groups with a maximum of 3.15 mM (56.8 mg/dL) on day 14 in T2DM subjects. LGD-6972 also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. LGD-6972 is well tolerated at the doses tested without dose-related or clinically meaningful changes in clinical laboratory parameters. No subject experiences hypoglycaemia[1].

[References]

[1]. Vajda EG, et al. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C₄₃H₄₆N₂O₅S

[ Molecular Weight ]:
702.901

[ Exact Mass ]:
702.312744

[ LogP ]:
8.45

[ Index of Refraction ]:
1.616

[ Storage condition ]:
2-8℃

Related Compounds

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