Cas No.: | 1207989-09-0 |
Synonyms: | LGD6972; LGD 6972 |
SMILES: | O=C(NCCS(=O)(O)=O)C1=CC=C(C[C@H](C2=CC=C(C3=CC=C(C(C)(C)C)C=C3)C=C2)C(NC4=CC=C(C5=C(C)C=C(C)C=C5C)C=C4)=O)C=C1 |
Formula: | C43H46N2O5S |
M.Wt: | 702.9 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. |
Description: | LGD-6972 is a glucagon receptor antagonist. |
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. |